PUBLICATIONS

 

 

243.      Lian, Y.; Bergman, R. G.; Ellman, J. A. "Rhodium(III)-Catalyzed Synthesis of Phthalides by Cascade Addition and Cyclization of Benzimidates with Aldehydes" Chem. Sci. 3, Advance Article (2012). ::doi::

 

242.      Verdoes, M.; Edgington, L. E.; Scheeren, F. A.; Leyva, M.; Blum, G.; Weiskopf, K.; Bachmann, M. H.; Ellman, J. A.; Bogyo, M. “A Nonpeptidic Cathepsin S Activity-Based Probe for Noninvasive Optical Imaging of Tumor-Associated Macrophages” Chem. Biol. 19, 619–628 (2012). ::doi::

 

241.     Kimmel, K. K.; Weaver, J. D.; Lee, M.; Ellman, J. A. “Enantio- and Diastereoselective Addition of Cyclohexyl Meldrum’s Acid to ß- and a,ß-Disubstituted Nitroalkenes via N-Sulfinyl Urea Catalysis” J. Am. Chem. Soc. 134, 9058–9061 (2012). ::doi::

 

240.      Xue, Y.; Chowdhury, S.; Liu, X.; Akiyama, Y.; Ellman, J. A.; Ha, Y. “Conformational Change in Rhomboid Protease GlpG Induced by Inhibitor Binding to Its S′ Subsites” Biochemistry 51, 3723–3731 (2012). ::doi::

 

239.      Hesp, K. D.; Bergman, R. G.; Ellman, J. A. “Rhodium-Catalyzed Synthesis of Branched Amines by Direct Addition of Benzamides to Imines” Org. Lett. 14, 2304-2307 (2012). ::doi::

 

238.      Martin, R. M.; Bergman, R. G.; Ellman, J. A. “Synthesis of Pyridines from Ketoximes and Terminal Alkynes via C–H Bond Functionalization” J. Org. Chem. 77, 2501–2507 (2012). ::doi::

 

237.      Duttwyler, S.; Rheingold, A. L.; Bergman, R. G.; Ellman, J. A. “Highly Diastereoselective Synthesis of Tetrahydropyridines by a C–H Activation–Cyclization–Reduction Cascade” J. Am. Chem. Soc. 134, 4064-4067 (2012). ::doi::

 

236.      Tauchert, M. E.; Incarvito, C. D.; Rheingold, A. L.; Bergman, R. G.; Ellman, J. A. “Mechanism of the Rhodium(III)-Catalyzed Arylation of Imines via C–H Bond Functionalization: Inhibition by Substrate” J. Am. Chem. Soc. 134, 1482–1485 (2012). ::doi::

 

235.      Kimmel, K. K.; Robak, M. T.; Thomas, S.; Lee, M. “Enantio- and Diastereoselective Addition of Thioacetic Acid to Nitroalkenes via N-Sulfinyl Urea Catalysis” Tetrahedron 68, 2704-2712 (2012). ::doi::

 

234.      Colby, D. A.; Tsai, A. S.; Bergman, R. G.; Ellman, J. A. “Rhodium Catalyzed Chelation-Assisted C–H Bond Functionalization Reactions” Acc. Chem. Res. 45, 814-825 (2012). ::doi::

 

233.      Kimmel, K.L.; Weaver, J.D.; Ellman, J.A. "Enantio- and Diastereoselective Addition of Cyclohexyl Meldrum's Acid to β- and α,β-Disubstituted Nitroalkenes via N-Sulfinyl Urea Catalysis” Chem. Science 3, 121-125 (2012). ::doi::

 

232.      Hesp, K.D.; Bergman, R.G.; Ellman, J.A. “Expedient Synthesis of N-Acyl Anthranilamides and β-Enamine Amides by the Rh(III)-Catalyzed Amidation of Aryl and Vinyl C-H Bonds with Isocyanates” J. Am. Chem. Soc. 133, 11430–11433 (2011). ::doi::

 

231.      Jung, H.H.; Buesking, A.W.; Ellman, J.A. “Highly Functional Group Compatible Rh-Catalyzed Addition of Arylboroxines to Activated N-tert-Butanesulfinyl Ketimines” Org. Lett. 13, 3912-1915 (2011). ::doi::

 

230.      Robak, M.T.; Herbage, M.A.; Ellman, J.A. “Development of an N-Sulfinyl Prolinamide for the Asymmetric Aldol Reaction” Tetrahedron 67, 4412-4416 (2011). ::doi:: [Dean Toste Tetrahedron Young Investigator Award Issue].

 

229.      Brasse, M.; Ellman, J.A.; Bergman, R.G. “A Facile, Metal- and Solvent Free, Autoxidative Coupling of Quinolines with Indoles and Pyrroles” Chem. Commun. 47, 5019-5021 (2011). ::doi::

 

228.      Mahajan, S. S.; Deu, E.; Lauterwasser, E. M. W.; Leyva, M. J.; Ellman, J. A.; Bogyo, M.; Renslo, A. R. “A Fragmenting Hybrid Approach for Targeted Delivery of Multiple Therapeutic Agents to the Malaria Parasite” ChemMedChem 6, 415–419 (2011). ::doi::

 

227.      Buesking, A. W.; Baguley, T. D.; Ellman, J. A. “Asymmetric Synthesis of Amines by the Knochel-Type MgCl2-Enhanced Addition of Benzyl Zinc Reagents to N-tert-Butanesulfinyl Aldimines” Org. Lett. 13, 964-967 (2011). ::doi::

 

226.      Tsai, A. S.; Tauchert, M. E.; Bergman, R. G.; Ellman, J. A. “Rhodium(III)-Catalyzed Arylation of Boc-Imines via CH Bond Functionalization” J. Am. Chem. Soc. 133, 1248–1250 (2011). ::doi::

 

225.      Tsai, A. S.; Brasse, M.; Bergman, R. G.; Ellman, J. A. “Rh(III)-Catalyzed Oxidative Coupling of Unactivated Alkenes via CH Activation” Org. Lett. 13, 540-542 (2011). ::doi::

 

224.      Floyd III, W. C.; Datta, G. K.; Imamura, S.; Kieler-Ferguson, H. M.; Jerger, K.; Patterson, A. W.; Fox, M. E.; Szoka, F. C.; Fréchet, J. M. J.; Ellman, J. A. “Chemotherapeutic Evaluation of a Novel Synthetic Tubulysin Analogue-Dendrimer Conjugate in C26 Tumor Bearing Mice” ChemMedChem 6, 49-53 (2011). ::doi:: [selected as Very Important Paper].

 

223.      Berman, A. M.; Bergman, R. G.; Ellman, J. A. “Rh(I)-Catalyzed Direct Arylation of Azines” J. Org. Chem. 75, 7863–7868 (2010). ::doi::

 

222.      Crimmin, M. R.; Colby, D. A.; Bergman, R. G.; Ellman, J. A. “Synthesis and Coordination Chemistry of Tri-Substituted Benzamidrazones” J. Chem. Soc., Dalton Trans. 40, 514-522 (2011). ::doi::

 

221.      Nichols, J. M.; Bishop, L. M.; Bergman, R. G.; Ellman, J. A. “Catalytic C-O Bond Cleavage of 2-Aryloxy-1-arylethanols and Its Application to the Depolymerization of Lignin Related Polymers” J. Am. Chem. Soc. 132, 12554-12555 (2010). ::doi::

 

220.      Datta, G. K.; Ellman, J. A. “Racemization Free Protocol for the Synthesis of N-tert-Butanesulfinyl Ketimimes” J. Org. Chem. 75, 6283-6285 (2010). ::doi::

 

219.      Leyva, M. J.; DeGiacomo, F.; Kaltenbach, L. S.; Holcomb, J.; Zhang, N.; Gafni, J.; Park, H.; Lo, D. C.;  Salvesen, G. S. Ellerby, L. M.; Ellman, J. A. “Identification and Evaluation of Novel Small Molecule Pan-Caspase Inhibitors in Huntington’s Disease Models” Chem. Biol. 17, 1189-1200 (2010). ::doi::

 

218.      Rawls, K. A.; Grundner, C.; Ellman, J. A. “Design and Synthesis of Novel Inhibitors for the Mycobacterium tuberculosis Phosphatase PtpB” Org. Biomol. Chem. 8, 4066-4070 (2010). ::doi::

 

217.      Deu, E.; Leyva, M.; Albrow, V.; Rice, M. J.; Ellman, J. A.; Bogyo, M. “Functional studies of the Plasmodium falciparum dipeptidyl aminopeptidase I (DPAP1) using small molecule inhibitors and active site” Chem. Biol. 17, 808-819 (2010). ::doi::

 

216.      Arceo, E.; Ellman, J. A.; Bergman, R. G. “Rhenium-Catalyzed Didehydroxylation of Vicinal Diols to Alkenes Using a Simple Alcohol as a Reducing Agent” J. Am. Chem. Soc. 132, 11408–11409 (2010). ::doi::

 

215.      Yotphan, S.; Bergman, R. G.; Ellman, J. A. “Synthesis of Multicyclic Pyridine and Quinoline Derivatives via Intramolecular C-H Bond Functionalization” Org. Lett. 12, 2978-2981 (2010). ::doi::

 

214.      Arceo, E.; Ellman, J. A.; Bergman, R. G. “A Direct, Biomass-Based Synthesis of Benzoic Acid: Formic Acid-mediated Deoxygenation of the Glucose-Derived Materials Quinic Acid and Shikimic Acid” ChemSusChem 3, 811–813 (2010). ::doi::

 

213.      Robak, M. T.; Herbage, M. A.; Ellman, J. A. “Synthesis and Applications of tert-Butanesulfinamide” Chem. Rev. 110, 3600–3740 (2010). ::doi::

 

212.      Brak, K.; Ellman, J. A. “Asymmetric Rh(I)-Catalyzed Addition of MIDA Boronates to N-tert-Butanesulfinyl Aldimines: Development and Comparison to Trifluoroborates” J. Org. Chem. 75, 3147–3150 (2010). ::doi::

 

211.      Brak, K.; Ellman, J. A. “Total Synthesis of (-)-Aurantioclavine” Org. Lett. 12, 2004–2007 (2010). ::doi::

 

210.      Brak, K.; Kerr, I. D.; Barrett, K. T.; Fuchi, N.; Debnath, M.; Ang, K.; Engel, J. C.; McKerrow, J. H.; Doyle, P. S.; Brinen, L. S.; Ellman, J. A. “Nonpeptidic Tetrafluorophenoxymethyl Ketone Cruzain Inhibitors as Promising New Leads for Chagas Disease Chemotherapy” J. Med. Chem. 53, 1763–1773 (2010). ::doi::

 

209.      Drag, M.; Bogyo, M.; Ellman, J. A.; Salvesen, G. S. “Aminopeptidase Fingerprints, an Integrated Approach for Identification of Good Substrates and Optimal Inhibitors”   J. Biol. Chem. 285, 3310-3318 (2010). ::doi::

 

208.      Sun, C.; Su, K.-H.; Valentine, J.; Rosa-Bauza, Y. T.; Ellman, J. A.; Elboudwarej, O.; Mukherjee, B.; Craik, C. S.; Shuman, M. A.; Chen, F. F.; Zhang, X. “Time-Resolved Single-Step Protease Activity Quantification Using Nanoplasmonic Resonator Sensors” ACS Nano 4, 978–984 (2010). ::doi::

 

207.      Colby, D. A.; Bergman, R. G.; Ellman, J. A. “Rhodium-Catalyzed C-C Bond Formation via Heteroatom-Directed C-H Bond Activation” Chem. Rev. 110, 624-655 (2010). ::doi::

 

206.      Storgaard, M.; Ellman, J. A. “Rhodium-Catalyzed Enantioselective Addition of Arylboronic Acids to In Situ Generated N-Boc Arylimines. Preparation of (S)-tert-Butyl (4-Chlorophenyl)(Thiophen-2-yl-MethyylCarbamate” Org. Synth. 86, 360-373 (2009).

 

205.      Rawls, K. A.; Lang, T. P.; Takeuchi, J.; Imamura, S.; Baguley, T. D.; Grundner, C.; Alber, T.; Ellman, J. A. “Fragment-based discovery of selective inhibitors of the Mycobacterium tuberculosis protein tyrosine phosphatase PtpA” Bioorg. Med. Chem. Lett. 19, 6851-6854 (2009). ::doi::

 

204.      Kimmel, K. L.; Robak, M. T.; Ellman, J. A. “Enantioselective Addition of Thioacetic Acid to Nitroalkenes via N-Sulfinyl Urea Organocatalysis” J. Am. Chem. Soc. 131, 8754–8755 (2009). ::doi::

 

203.      Arceo, E.; Marsden, P.; Bergman, R. G.; Ellman, J. A. “An Efficient Didehydroxylation Method for the Biomass-Derived Polyols Glycerol and Erythritol. Mechanistic Studies of a Formic Acid-Mediated Deoxygenation” Chem. Commun. 3357-3359 (2009). ::doi::

 

202.      Tsai, A. S.; Wilson, R. M.; Hirada, H.; Bergman, R. G.; Ellman, J. A. “Rhodium Catalyzed Enantioselective Cylization of Substituted Imidazoles via C–H Bond Activation” Chem. Commun. 3910-3912 (2009). ::doi::

 

201.      Brak, K.; Harris, K. ; Ellman, J. A. “General One-pot Method for the Preparation of N-tert-Butanesulfinyl Amine Diastereomer Mixtures as Standards for Stereoselectivity Determinations” J. Org. Chem. 74, 3606-3608 (2009). ::doi::

 

200.      Brak, K.; Ellman, J. A. “Asymmetric Synthesis of α–Branched Allylic Amines by the Rh(I)-Catalyzed Addition of Alkenyltrifluoroborates to N-tert-Butanesulfinyl Aldimines” J. Am. Chem. Soc. 131, 3850–3851 (2009). ::doi::

 

199.      Yotphan, S.; Bergman, R. G.; Ellman, J. A. “Application of Daugulis Copper-Catalyzed Direct Arylation to the Synthesis of 5-Aryl Benzotriazepines” Org. Lett. 11, 1511–1514 (2009). ::doi::

 

198.      Wakayama , M.; Ellman, J. A. “Recycling the tert-Butanesulfinyl Group in the Synthesis of Amines Using tert-Butanesulfinamide” J. Org. Chem. 74, 2646–2650 (2009). ::doi:: [JOC Feature article and highlighted by Trevor Laird and coauthors in Org. Proc. Res. Dev. 2009, 13, 364–370].

 

197.      Berman, A. M.; Lewis, J. C.; Bergman, R. G.; Ellman, J. A. “Rh(I)-Catalyzed Direct Arylation of Pyridines and Quinolines” J. Am. Chem. Soc. 130, 14926–14927 (2008). ::doi::

 

196.      Harada, H.; Thalji, R. K.; Bergman, R. G.; Ellman, J. A. “Enantioselective Intramolecular Hydroarylation of Alkenes via Directed C-H Bond Activation” J. Org. Chem. 73, 6772-6779 (2008). ::doi::

 

195.      Lewis, J. C.; Bergman, R. G.; Ellman, J. A. “Direct Functionalization of Nitrogen Heterocycles via Rh-Catalyzed C-H Bond Activation” Acc. Chem. Res. 41, 1013-1025 (2008). ::doi::

 

194.      Drag, M.; Mikolajczyk, J.; Bekes, M.; Reyes-Turcu, F.; Ellman, J. A.; Wilkinson, K. D.; Salvesen, G. S. “Positional-Scanning Fluorogenic Substrate Libraries Reveal Unexpected Specificity Determinants of Deubiquitinating Enzymes (DUBs)” Biochem. J. 415, 367-375 (2008). ::doi::

 

193.      Trincado, M.; Ellman, J. A. “Enantioselective Synthesis of alpha-Aryl Alkylamines by Rh-Catalyzed Addition Reactions of Arylboronic Acids to Aliphatic Imines” Angew. Chem. Int. Ed. 47, 5623-5626 (2008). ::doi::

 

192.      Beenen, M. A.; An, C.; Ellman, J. A. “Asymmetric Copper-Catalyzed Synthesis of alpha-Amino Boronate Esters from N-tert-Butanesulfinyl Aldimines” J. Am. Chem. Soc. 130, 6910-6911 (2008). ::doi::

 

191.      Patterson, A. W.; Peltier, H. M.; Ellman, J. A. “Expedient Synthesis of N-Methyl Tubulysin Analogues with High Cytotoxicity” J. Org. Chem. 73, 4362-4369 (2008). ::doi::

 

190.      Gribble, M. W.; Ellman, J. A.; Bergman, R. G. “Synthesis of a Benzodiazepine-Derived Rhodium NHC Complex by C-H Bond Activation” Organometallics, 27, 2152-2155 (2008). ::doi::

 

189.      Brak, K.; Doyle, P. S.; McKerrow, J. H.; Ellman, J. A. “Identification of a New Class of Nonpeptidic Inhibitors of Cruzain” J. Am. Chem. Soc. 130, 6404-6410 (2008). ::doi::

 

188.      Tsai, A. S.; Bergman, R. G.; Ellman, J. A. “Asymmetric Synthesis of (−)-Incarvillateine Employing an Intramolecular Alkylation via Rh-Catalyzed Olefinic C−H Bond Activation” J. Am. Chem. Soc. 130, 6316-6317 (2008). ::doi::

 

187.      Colby, D. A.; Bergman, R. G.; Ellman, J. A. “Synthesis of Dihydropyridines and Pyridines from Imines and Alkynes via C-H Activation” J. Am. Chem. Soc. 130, 3645-3651 (2008). ::doi::

 

186.      Yotphan, S.; Bergman, R. G.; Ellman, J. A. “The Stereoselective Formation of Bicyclic Enamines with Bridgehead Unsaturation via Tandem C-H Bond Activation/Alkenylation/Electrocyclization” J. Am. Chem. Soc. 130, 2452-2453 (2008). ::doi::

 

185.      Lewis, J. C.; Berman, A. M.; Bergman, R. G.; Ellman, J. A. “Rh(I)-Catalyzed Arylation of Heterocycles via C-H Bond Activation:  Expanded Scope Through Mechanistic Insight.” J. Am. Chem. Soc. 130, 2493-2500 (2008). ::doi::

 

184.      Robak, M. T.; Trincado, M.; Ellman, J. A. “Enantioselective Aza-Henry Reaction with an N-Sulfinyl Urea Organocatalyst” J. Am. Chem. Soc. 129, 15110-15111 (2007). ::doi::

 

183.      Nakagawa, H.; Rech, J. C.; Sindelar, R. W.; Ellman, J. A. “Catalytic Enantioselective Addition of Arylboronic Acids to N-Boc Imines Generated in Situ” Org. Lett. 9, 5155-5157 (2007). ::doi::

 

182.      Patterson, A. W.; Peltier, H. M.; Sasse, F.; Ellman, J. A. “Design, Synthesis, and Biological Properties of Highly Potent Tubulysin D Analogues” Chem. Eur. J. 13, 9534-9541 (2007). ::doi::

 

181.      Tanuwidjaja, J.; Peltier, H. M.; Lewis, J. C.; Schenkel, L. B.; Ellman, J. A. “One-Pot Microwave-Promoted Synthesis of Nitriles from Aldehydes via tert-Butanesulfinyl Imines” Synthesis 3385-3389 (2007). ::doi::

 

180.      Watzke, A.; Wilson, R. M.; O’Malley, S. J.; Bergman, R. G.; Ellman, J. A. “Asymmetric Intramolecular Alkylation of Chiral Aromatic Imines via Catalytic C-H Bond Activation” Synlett 2383-2389 (2007). ::doi::

 

179.      Soellner, M. B.; Rawles, K. A.; Grundner, C.; Alber, T.; Ellman, J. A. “Fragment-Based Substrate Activity Screening Method for the Identification of Potent Inhibitors of the M. tuberculosis Phosphatase PtpB” J. Am. Chem. Soc.  129, 9613-9615 (2007). ::doi:: [Research Highlight in Nat. Chem. Biol. 3, 539 (2007)].

 

178.      Rosa-Bauza, Y. T.; Berst, F.; Ellman, J. A. “Straightforward Preparation and Assay of Aspartyl Protease Substrates with an Internal Thioester Linkage” ChemBioChem 8, 981-984 (2007). ::doi::

 

177.      Ellman, J. A. “The Direct Approach” Science 316, 1131-1132 (2007). ::doi::

 

176.      Inagaki, H.; Tsuruoka, H.; Hornsby, M.; Lesley, S. A.; Spraggon, G.; Ellman, J. A. “Nonpeptidic Inhibitors of Cathepsin S with an Unprecedented Binding Mode” J. Med. Chem. 50, 2693-2699 (2007). ::doi::

 

175.      Lewis, J. C.; Bergman, R. G.; Ellman, J. A. “Rh(I)-Catalyzed Alkylation of Quinolines and Pyridines via C-H Bond Activation” J. Am. Chem. Soc. 129, 5332-5333 (2007). ::doi::

 

174.      Rech, J. C.; Yato, M.; Duckett, D.; Ember, Brian; LoGrasso, P. V.; Bergman, R. G.; Ellman, J. A. “Synthesis of Potent Bicyclic Bisarylimidazole c-Jun N-Terminal Kinase Inhibitors by Catalytic C-H Bond Activation” J. Am. Chem. Soc. 129, 490-491 (2007). ::doi::

 

173.      Tanuwidjaja, J.; Peltier, H. M.; Ellman, J. A. “One-Pot Asymmetric Synthesis of Either Diastereomer of tert-Butanesulfinyl-protected Amines from Ketones” J. Org. Chem. 72, 626-629 (2007). ::doi::

 

172.      Liu, G. L.; Rosa-Bauza, Y. T.; Salisbury, C. T.; Lu, Y.; Kim, J.; Craik, C.; Ellman, J. A.; Lee, L. P.; Chen, F. F. "Peptide-Nanocrescent Hybrid SERS Probe for Optical Detection of Protease Activity" J.  Nanoscience Nanotech. 7, 2323–2330 (2007). ::doi::

 

171.      Peltier, H. M.; McMahon, J. P.; Patterson, A. W.; Ellman, J. A. “The Total Synthesis of Tubulysin D” J. Am. Chem. Soc. 128, 16018-16019 (2006). ::doi:: Critique: Sasse, F.; Menche, D. “Success in Tubulysin D Synthesis” Nat. Chem. Biol. 3, 87-89 (2007).

 

170.      Patterson, A. W.; Wood, W. J. L.; Ellman, J. A. “Substrate Activity Acreening (SAS): a General Procedure for the Preparation and Screening of a Fragment-Based Non-Peptidic Protease Substrate Library for Inhibitor Discovery” Nature Protocols 2, 424 - 433 (2007). ::doi::

 

169.      Patterson, A. W.; Wood, W. J. L.; Hornsby, M.; Lesley, S.; Spraggon, G.; Ellman, J. A. “Identification of Selective, Nonpeptidic Nitrile Inhibitors of Cathepsin S using the Substrate Activity Screening Method” J. Med. Chem. 49, 6298-6307 (2006). ::doi::

 

168.      Watzke, A.; O’Malley, S. J.; Bergman, R. G.; Ellman, J. A. “Reassignment of Configuration for Salvianolic Acid B and Establishment of Its Identity with Lithospermic Acid B” J. Nat. Prod. 69, 1231-1233 (2006). ::doi::

 

167.      Patterson, A. W.; Ellman, J. A. “Asymmetric Synthesis of alpha,alpha-Dibranched Propargylamines by Acetylide Additions to N-tert-Butanesulfinyl Ketimines” J. Org. Chem. 71, 7110-7112 (2006). ::doi::

 

166.      Salisbury , C. M.; Ellman, J. A. “Rapid Identification of Potent Nonpeptidic Serine Protease Inhibitors” ChemBioChem 7, 1034-1037 (2006). ::doi::

 

165.      Zhang, Y.; Lewis, J. C.; Bergman, R. G.; Ellman, J. A.; Oldfield, E. “NMR Shifts, Orbitals, and M···H-X Bonding in d8 Square Planar Metal Complexes” Organometallics 25, 3515-3519 (2006). ::doi::

 

164.      Choe, Y.; Leonetti, F.; Greenbaum, D. C.; Lecaille, F.; Bogyo, M.; Bromme, D.; Ellman, J. A.; Craik, C. S. “Substrate Profiling of Cysteine Proteases Using a Combinatorial Peptide Library Identifies Functionally Unique Specificities” J. Biol. Chem. 281, 12824 - 12832 (2006). ::doi::

 

163.      Gosalia D.N.; Denney, W. S.; Salisbury, C. M.; Ellman, J. A.; Diamond, S. L. “Functional Phenotyping of Human Plasma Using a 361-Fluorogenic Substrate Biosensing Microarray” Biotechnol. Bioeng. 94, 1099-1110 (2006). ::doi::

 

162.      Wilson, R. M.; Thalji, R. K.; Bergman, R. G.; Ellman, J. A. “Enantioselective Synthesis of a PKC Inhibitor via Catalytic C-H Bond Activation” Org. Lett. 8, 1745-1747 (2006). ::doi::

 

161.      Beenen, M. A.; Weix, D. J.; Ellman, J. A. “Asymmetric Synthesis of Protected Arylglycines by Rhodium-Catalyzed Addition of Arylboronic Acids to N-tert-Butanesulfinyl Imino Esters” J. Am. Chem. Soc. 128, 6304-6305 (2006). ::doi::

 

160.      Colby, D. A.; Bergman, R. G.; Ellman, J. A. “Stereoselective Alkylation of alpha,beta-Unsaturated Imines via C-H Bond Activation” J. Am. Chem. Soc. 128, 5604-05 (2006). ::doi::

 

159.      Lewis, J. C.; Wu, J. Y.; Ellman, J. A.; Bergman, R. G. “Microwave-Promoted Rhodium-Catalyzed Arylation of Heterocycles through CH Bond Activation” Angew. Chem. Int. Ed. 45, 1589-1591 (2006). ::doi::

 

158.      Wiedemann, S. H.; Lewis, J. C.; Ellman, J. A.; Bergman, R. G. “Experimental and Computational Studies on the Mechanism of N-Heterocycle C-H Activation by Rh(I)” J. Am. Chem. Soc. 128, 2452-2462 (2006). ::doi::

 

157.      Wiedemann, S. H.; Ellman, J. A.; Bergman, R. G. “Rhodium-Catalyzed Direct C-H Addition of 3,4-Dihydroquinazolines to Alkenes and Their Use in the Total Synthesis of Vasicoline” J. Org. Chem. 71, 1969-1976 (2006). ::doi::

 

156.      Wood, W. J. L.; Patterson, A. W.; Tsuruoka, H.; Jain, R. K.; Ellman, J. A. “Substrate Activity Screening: A Fragment-Based Method for the Rapid Identification of Nonpeptidic Protease Inhibitors” J. Am. Chem. Soc. 127,s:.25in 27.0pt list 40.5pt left 1.0in 1.5in 2.0in 2.5in 3.0in 3.5in 4.0in 4.5in 5.0in 5.5in 6.0in 6.5in">

Nat. Chem. Biol. 1, 359 (2005)]. 155.      McMahon, J. P.; Ellman, J. A. “Asymmetric Conjugate Addition of Copper Reagents to alpha,beta-Unsaturated tert-Butanesulfinyl Imines” Org. Lett. 7, 5393-5396 (2005). ::doi::

 

154.      Weix, D. J.; Ellman, J. A. “(+)-2-Methyl-2-propanesulfinamide” Org. Synth. 82, 157-165 (2005).

 

153.      Lewis, J. C.; Wu, J.; Bergman, R. G.; Ellman, J. A. “Preagostic Rh-H Interactions and C-H Bond Functionalization: A Combined Experimental and Theoretical Investigation of Rhodium(I) Phosphinite Complexes” Organometallics 24, 5737-5746 (2005). ::doi::

 

152.      O'Malley, S. J.; Tan, K. L.; Watzke, A.; Bergman, R. G.; Ellman, J. A. “Total Synthesis of (+)-Lithospermic Acid by Asymmetric Intramolecular Alkylation via Catalytic C-H Bond Activation” J. Am. Chem. Soc. 127, 13496-13497 (2005). ::doi::

 

151.      Peltier, H. M.; Ellman, J. A. “N-Sulfinyl Metalloenamine Conjugate Additions: Asymmetric Synthesis of Piperidines” J. Org. Chem. 70, 7342-7345 (2005). ::doi::

 

150.      Thalji, R. K.; Ahrendt, K. A.; Bergman, R. G.; Ellman, J. A. “Annulation of Aromatic Imines via Directed C-H Bond Activation”  J. Org. Chem. 70, 6775-6781 (2005). ::doi::

 

149.      Brinner, K. M.; Ellman, J. A.  “A Rapid and General Method for the Asymmetric Synthesis of 2-Substituted Pyrrolidines Using tert-Butanesulfinamide” Org. Biomol. Chem. 3, 2109-2113 (2005). ::doi::

 

148.      Ghosalia, D. N.; Salisbury, C. M.; Maly, D. J.; Ellman, J. A.;  Diamond, S. L. “Profiling Serine Protease Substrate Specificity with Solution Phase Fluorogenic Peptide Microarrays” Proteomics 5, 1292-1298 (2005). ::doi::

 

147.      Wiedemann, S. H.; Ellman, J. A.; Bergman, R. G. Catalytic Functionalization of N-Heterocycles via their Rhodium-Carbene Complexes. In Handbook of C-H Transformations; Dyker, G., Ed.: Wiley-VCH Verlag GmbH & Co. KGaA; Weinheim, 187-193 (2005).

 

146.      Gosalia, D. N.; Salisbury, C. M.; Ellman, J. A.; Diamond, S. L. “High Throughput Substrate Specificity Profiling of Serine and Cysteine Proteases Using Solution-Phase Fluorogenic Peptide Microarays” Molec. Cell. Proteomics 4, 626-636 (2005). ::doi::

 

145.      Peltier, H. M.; Evans, J. W.; Ellman, J. A. “Catalytic Enantioselective Sulfinyl Transfer Using Cinchona Alkaloid Catalysts” Org. Lett. 7, 1733-1736 (2005). ::doi::

 

144.      Brinner, K.; Ellman, J. A. Asymmetric Synthesis of  beta-Amino Acids by Enolate Additions to tert-Butanesulfinyl Imines. In Enantioselective  Synthesis of b-Amino Acids, 2nd Edition; Juaristi, E., Soloshonok, V.,  Eds.; John Wiley & Sons, Hoboken, NJ; pp 181-194 (2005).

 

143.      Brinner, K. M.; Powles, M. A.; Schmatz, D. M.; Ellman, J. A. “Potent 4-Aminopiperidine Based Antimalarial Agents” Bioorg. Med. Chem. Lett. 15, 345-348 (2005). ::doi::

 

142.      Weix, D. J.; Shi, Y.; Ellman, J. A. “Diastereoselective and Enantioselective Rh(I)-Catalyzed Additions of Arylboronic Acids to N-tert-Butanesulfinyl and N-Diphenylphosphinoyl Aldimines” J. Am. Chem. Soc.  127, 1092-1093 (2005). ::doi::

 

141.      Kochi , T.; Ellman, J. A. “Asymmetric alpha-Alkylation of N'-tert-Butanesulfinyl Amidines. Application to the Total Synthesis of (6R,7S)-7-Amino-7,8-dihydro-alpha-bisabolene” J. Am. Chem. Soc.  126, 15652-15653 (2004). ::doi::

 

140.      Tan, K. L.; Park, S.; Ellman, J. A.; Bergman, R. G. “Intermolecular Coupling of Alkenes to Heterocycles via C-H Bond Activation” J. Org. Chem. 69, 7329-7335 (2004). ::doi::

 

139.      Evans, J .W.; Fierman, M. B.; Miller, S. J.; Ellman, J. A. “Catalytic Enantioselective Synthesis of Sulfinate Esters Through the Dynamic Resolution of tert-Butanesulfinyl Chloride” J. Am. Chem. Soc.  126, 8134-8135 (2004).

 

138.      Schenkel, L. B.; Ellman, J.  A. “Self-Condensation of N-tert-Butanesulfinyl Aldimines: Application to the Asymmetric Synthesis of Biologically Important Amine-Containing Compounds” Org. Lett. 6, 3621-3624 (2004). ::doi::

 

137.      Klei, Steven R.; Tan, Kian L.; Golden, Jeffrey T.; Yung, Cathleen M.; Thalji, Reema K.; Ahrendt, Kateri A.; Ellman, Jonathan A.; Tilley, T. Don; Bergman, Robert G. R. C-H Bond activation by iridium and rhodium complexes: Catalytic hydrogen-deuterium exchange and C-C bond-forming reactions. In Activation and Functionalization of C-H Bonds; Goldberg, K. I.; Goldman, A. S., Ed.; ACS Symposium Series 885; American Chemical Society; Washington, DC, 46-55 (2004).

 

136.      Thalji, R. K.; Ellman, J. A.; Bergman, R. G. “Highly Efficient and Enantioselective Cyclization of Aromatic Imines via Directed C-H Bond Activation” J. Am. Chem. Soc. 126, 7192-7193 (2004). ::doi::

 

135.      Kochi , T.; Mukade, T. “Asymmetric Synthesis of Amines with tert-Butanesulfinamide and Its Application” J. Syn. Org. Chem. Jpn. 62, 128-139 (2004). ::doi::

 

134.      McMahon, J. P.; Ellman, J. A. “Highly Stereoselective Addition of Organometallic Reagents to N-tert-Butanesulfinyl Imines Derived from 3- and 4-Substituted Cyclohexanones” Org. Lett. 6, 1645-1647 (2004). ::doi::

 

133.      Wiedemann, S. H.; Bergman, R. G.; Ellman, J. A. “Rhodium-Catalyzed Direct C-H Addition of 4,4-Dimethyl-2-oxazoline to Alkenes” Org. Lett. 6, 1685-1687 (2004). ::doi::

 

132.      Schenkel, L. B.; Ellman, J. A. “Application of P,N-Sulfinyl Imine Ligands to Iridium-Catalyzed Asymmetric Hydrogenation of Olefins” J. Org. Chem. 69, 1800-1802 (2004). ::doi::

 

131.      Lewis, J. C. Wiedemann, S. H.; Bergman, R. G.; Ellman, J. A. “Arylation of Heterocycles via Rhodium-Catalyzed C-H Bond Functionalization::doi::” Org. Lett. 6, 35-38 (2004). ::doi::

 

130.      Evans, J. W.; Ellman, J. A. “Stereoselective Synthesis of 1,2-Disubstituted beta-Amino Alcohols by Nucleophilic Addition to N-tert-Butanesulfinyl aldimines” J. Org. Chem. 68, 9948-9957 (2003). ::doi::

 

129.      Wood, W.; Huang, L.; Ellman, J. A. “Synthesis of a Diverse Library of Mechanism-Based Cysteine Protease Inhibitors” J. Comb. Chem. 5, 869-880 (2003). ::doi::

 

128.      Boitano, A.; Ellman, J. A.; Glick, G. D.; Opipari, A. W. “The Proapoptotic Benzodiazepine BZ-423 Affects the Growth and Survival of Malignant B Cells” J. Cancer Res. 63, 6870-6876 (2003).

 

127.      Boitano, A.; Leonetii, F.; Emal, C.; Ellman, J. A.; Roush, W. R.; Opipari, A. W.; Glick, G. D. “Structure Activity Studies of a Novel Cytotoxic Benzodiazepine” Bioorg. Med. Chem. Lett.13, 3327-3330 (2003). ::doi::

 

126.      Kochi, T.; Tang, T. P.; Ellman, J. A. "Development and Application of a New General Method for the Asymmetric Synthesis of syn- and anti-1,3-Amino Alcohols" J. Am. Chem. Soc. 125, 11276-11282 (2003).

 

125.      Jain, R. K.; Trias, J.; Ellman, J. A. “D-Ala-D-Lac Binding is Not Required for the High Activity of Vancomycin Dimers Against Vancomycin Resistant Enterococci” J. Am. Chem. Soc. 125, 8740-8741 (2003). ::doi::

 

124.      Mukade, T.; Dragoli, D. R.; Ellman, J. A. “Parallel Solution-Phase Asymmetric Synthesis of alpha-Branched Amines” J. Comb. Chem. 5, 590-596 (2003). ::doi::

 

123.      Tan, K. L.; Vasudevan, A.; Bergman, R. G.; Ellman, J. A.; Souers, A. J. “Microwave Assisted C-H Bond Activation: A Rapid Entry into Functionalized Heterocycles” Org. Lett. 5, 2131-2134 (2003). ::doi::

 

122.      Ahrendt, K. A.; Bergman, R. G.; Ellman, J. A. “Synthesis of a Tricyclic Mescaline Analog by Catalytic C-H Bond Activation” Org. Lett. 5, 1301-1303 (2003). ::doi::

 

121.      Weix, D. J.; Ellman, J. A. “An Improved Synthesis of tert-Butanesulfinamide Suitable for Large Scale Production” Org. Lett. 5, 1317-1320 (2003). ::doi::

 

120.      Leiting, B.; Pryor, K. D.; Wu, J. K.; Marsilio, F.; Patel, R. A.; Craik, C. S.; Ellman, J. A.; Cummings, R. T.; Thornberry, N. “Catalytic Properties and Inhibition of Proline-Specific Dipeptidyl Peptidases II, IV and VII” Biochem. J. 371, 525-532 (2003). ::doi::

 

119.      Ahrendt, K. A.; Olsen, J. A.; Wakao, M.; Trias, J. Ellman, J. A. “Identification of Potent and Broad-Spectrum Antibiotics from SAR Studies of a Synthetic Vancomycin Analog” Bioorg. Med. Chem. Lett. 13, 1683-1686 (2003). ::doi::

 

118.      Cawley, N. X.; Chino, M.; Maldonado, A.; Rodriguez, Y. M.; Loh, Y. P.; Ellman, J. A. “Synthesis and Characterization of the First Potent Inhibitor of Yapsin 1. Implications for the Study of Yapsin-Like Enzymes” J. Biol. Chem. 278, 5523-5530 (2003). ::doi::

 

117.      Asojo, O. A.; Gulnik. S. V.; Afonina, E.; Yu, B.; Ellman, J. A.; Haque, T. S.; Silva, A. M. “Novel Uncomplexed and Complexed Structures of Plasmepsin II, an Aspartic Protease from Plasmodium falciparum” J. Mol. Biol. 327, 173-181 (2003). ::doi::

 

116.      Schenkel, L. B.; Ellman, J. A. “Novel Sulfinyl Imine Ligands for Asymmetric Catalysis” Org. Lett. 5, 545-548 (2003). ::doi::

 

115.      Bednarski, J. J.; Warner, R. E.; Rao, T.; Leonetti, F.; Yung, R.; Richardson, B. C.; Johnson, K. J.; Ellman, J. A. Opipari, A. W.; Glick, G. D. “Attenuation of Autoimmune Disease in Fas-Deficient Mice by Treatment with a Cytotoxic Benzodiazepine” Arthritis & Rheumatism  48, 757-766 (2003). ::doi::

 

114.      Huang, L.; Brinen, L. S.; Ellman, J. A. “ Crystal Structures of Reversible Ketone-Based Inhibitors of the Cysteine Protease Cruzain” Bioorg. Med. Chem. 11, 21-29 (2003). ::doi::

 

113.      Ellman, J. A. “Applications of tert-Butanesulfinamide in the Asymmetric Synthesis of Amines” Pure Appl. Chem. 75, 39-46 (2003). ::doi::

 

112.      Owens, T. D.; Souers, A. J.; Ellman, J. A. “The Preparation and Utility of Bis(sulfinyl)imidoamidine Ligands for the Copper-Catalyzed Diels Alder Reaction” J. Org. Chem. 68, 3-10 (2003). ::doi::

 

111.      Blum, S. A.; Bergman, R. G.; Ellman, J. A. “Enantioselective Oxidation of Di-tert-Butyl Disulfide with a Vanadium Catalyst: Progress toward Mechanism Elucidation” J. Org. Chem. 68, 150-155 (2003). ::doi::

 

110.      Salisbury , C. M.; Maly, D. J.; Ellman, J. A. “Peptide Microarrays for the Determination of Substrate Specificity” J. Am. Chem. Soc. 124, 14868-14870 (2002). ::doi::

 

109.      Ellman, J. A.; Owens, T. D.; Tang, T. P. “N-tert-Butanesulfinyl Imines: Versatile Intermediates for the Asymmetric Synthesis of Amines” Acc. Chem. Res. 35, 984-995 (2002). ::doi::

 

108.      Tang, T. P.; Ellman, J. A. “Asymmetric Synthesis of beta-Amino Acid Derivatives Incorporating a Broad Range of Substitution Patterns by Enolate Additions to tert-Butanesulfinyl Imines” J. Org. Chem. 67, 7819-7832 (2002). ::doi::

 

107.      Blatt, N. B.; Bednarski, J. J.; Warner, R. E.; Leonetti, F.; Johnson, K. M.; Boitano, A.; Yung, R.; Richardson, B. C.; Johnson, K. J.; Ellman, J. A. Opipari, A. W.; Glick, G. D. “Benzodiazepine-Induced Superoxide Signals B Cell Apoptosis: Mechanistic Insight and Potential Therapeutic Utility” J. Clin. Invest. 110, 1123-1132 (2002). ::doi::

 

106.      Tan, K. L.; Bergman, R. G.; Ellman, J. A. “Intermolecular Coupling of Alkenes to Heterocycles via Rhodium-Catalyzed C-H Bond Activation” J. Am. Chem. Soc. 124, 13964-13965 (2002). ::doi::

 

105.      Huang, L.; Ellman, J. A. “General Solid-Phase Procedure to Prepare Novel Cyclic Ketone Inhibitors of the Cysteine Protease Cruzain” Bioorg. Med. Chem. Lett. 12, 2993-2996 (2002). ::doi::

 

104.      Choi, C. Y. H.; Schneider, E. L.; Kim, J. M.; Gluzman, I. Y.; Goldberg, D. E.; Ellman, J. A.; Marletta, A. “Interference with Heme Binding to Histidine-Rich Protein-2 As an Antimalarial Strategy” Chem. Biol. 9, 881-889 (2002). ::doi::

 

103.      Chino, M.; Wakao, M.; Ellman, J. A. “Efficient Method to Prepare Hydroxyethylamine-Based Aspartyl Protease Inhibitors with Diverse P1 Side Chains” Tetrahedron 58, 6305-6310 (2002). ::doi::

 

102.      Brinner, K. M.; Kim, J. M.; Habashita, H.; Gluzman, I. Y.; Goldberg, D. E.; Ellman, J. A. “Novel and Potent Anti-Malarial Agents” Bioorg. Med. Chem. 10, 3649-3661 (2002). ::doi::

 

101.      Kochi, T.; Tang, T. P.; Ellman, J. A. “Asymmetric Synthesis of syn- and anti-1,3-Amino Alcohols” J. Am. Chem. Soc. 124, 6518-6519 (2002). ::doi::

 

100.      Wang, X.; Choe, Y.; Craik, C. S.; Ellman, J. A. “Design and Synthesis of Novel Inhibitors of Gelatinase B” Bioorg. Med. Chem. Lett. 12, 2201-2204 (2002). ::doi::

 

99.      Tan, K. L.; Bergman, R. G.; Ellman, J. A. “Intermediacy of an N-Heterocyclic Carbene in the Catalytic C-H Activation of Benzimidazole” J. Am. Chem. Soc. 124, 3202-3203 (2002). ::doi::

 

98.      Kehoe, J. W.; Maly, D. J.; Verdugo, D. E.; Armstrong, J. I.; Cook, B. N.; Ouyang, Y.-B.; Moore, K. L.; Ellman, J. A.; Bertozzi, C. R. “Tyrosylprotein Sulfotransferase Inhibitors Generated by Combinatorial Target-Guided ligand Assembly” Bioorg. Med. Chem. Lett 12, 329-332 (2002). ::doi::

 

97.      Maly, D. J.; Leonetti, F.; Backes, B. J.; Dauber, D. S.; Harris, J. L.; Craik, C. S.; Ellman, J. A.  “Expedient Solid-Phase Synthesis of Fluorogenic Protease Substrates Using the 7-Amino-4-Carbamoylmethylcoumarin (ACC) Fluorophore” J. Org. Chem. 67, 910-915 (2002). ::doi::

96.      Maly, D. J.; Huang, L.; Ellman, J. A. “Combinatorial Strategies for Targeting Protein Families.  Application to the Proteases” ChemBioChem 3, 16-37 (2002). ::doi::

 

95.      Huang, L.; Lee, A.; Ellman, J. A. “Identification of Potent and Selective Mechanism-Based Inhibitors of the Cysteine Protease Cruzain Using Solid-Phase Parallel Synthesis” J. Med. Chem. 45, 676-684 (2002). ::doi::

 

94.      Dauber, D. S.; Ziermann, R. Parkin, N.; Maly, D. J.; Mahrus, S.; Harris, J. L.; Ellman, J. A.; Petropoulos, C.; Craik, C. S. “Altered Substrate Specificity of Drug-Resistant Human Immunodeficiency Virus Type 1 Protease” J. Virol. 76, 1359-1368 (2002). ::doi::

 

93.      Lee. A.; Ellman, J. A. “Parallel Solution-Phase Synthesis of Mechanism-Based Cysteine Protease Inhibitors” Org. Lett. 3, 3707-3709 (2001). ::doi::

 

92.      Tang, T. P.; Volkman, S. K.; Ellman, J. A. “Asymmetric Synthesis of 1,2-Amino Alcohols Using tert-Butanesulfinyl Aldimines and Ketimines” J. Org. Chem. 66, 8772-8778 (2001). ::doi::

 

91.      Thalji, R.; Ahrendt, K. A.; Bergman, R. G.; Ellman, J. A. “Annulation of Aromatic Imines via Directed C-H Activation with Wilkinson’s Catalyst” J. Am. Chem. Soc. 123, 9692-9693 (2001). ::doi::

 

90.      Souers, A. J.; Ellman, J. A. “beta-Turn Mimetic Library Synthesis: Scaffolds and Applications” Tetrahedron 57, 7431-7448 (2001). ::doi::

 

89.      Souers, A. J.; Owens, T. D.; Oliver, A. G.; Hollander, F. J.; Ellman, J. A. “Synthesis and Crystal Structure of a Unique and Homochiral N,S-Bonded N,N-Bis(-tert-Butanesulfinyl)amidinate Rhodium(I) Complex” Inorg. Chem.  40, 5299-5301 (2001). ::doi::

 

88.      Dragoli, D. R.; Burdett, M. T.; Ellman, J. A. “Design, Synthesis, and Utility of Support-Bound tert-Butanesulfinamide” J. Am. Chem. Soc. 123, 10127-10128 (2001). ::doi::

 

87.      Harris, J. L.; Niles, A.; Burdick, K.; Maffitt, M.; Backes, B. J.; Ellman, J. A.; Kuntz, I.; Haak-Frendscho, M.; Craik, C. S. “Definition of the Extended Substrate Specificity Determinants for beta-Tryptases I and II” J. Biol. Chem. 276, 34941-34947 (2001). ::doi::

 

86.      Tan, K. L.; Bergman, R. G.; Ellman, J. A. “Annulation of Alkenyl-Substituted Heterocycles via Rhodium-Catalyzed Intramolecular C-H Activated Coupling Reactions” J. Am. Chem. Soc. 123, 2685-2686 (2001). ::doi::

 

85.      Borg, G.; Chino , M.; Ellman, J. A. “Asymmetric Synthesis of Pre-Protected alpha,alpha-Disubstituted Amino Acids from tert-Butanesulfinyl Ketimines” Tetrahedron Lett. 42, 1433-1436 (2001). ::doi::

 

84.      Owens, T. D.; Hollander, F. J.; Oliver, A. G.; Ellman, J. A. “Synthesis, Utility, and Structure of Novel Bis(sulfinyl)imidoamidine Ligands for Asymmetric Lewis Acid Catalysis” J. Am. Chem. Soc. 123, 1539-1540 (2001). ::doi::

 

83.      Szewczyk, J. W.; Zuckermann, R. L.; Bergman, R. G.; Ellman, J. A. “A Mass Spectrometric Labeling Strategy for High-Throughput Reaction Evaluation and Optimization: Exploring C–H Activation” Angew. Chem. Int. Ed. 40, 216-219 (2001). ::doi::

 

82.      Backes, B. J.; Harris, J. L.; Leonetti, F.; Ellman, J. A.; Craik, C. “Rapid and General Profiling of Protease Specificity by Using Combinatorial Fluorogenic Substrate Libraries” Proc. Natl. Acad. Sci. 97, 7754-7759 (2000).

 

81.      Souers, A. J.; Rosenquist, A.; Jarvie, E. M.; Ladlow, M.; Fenuik, W.; Ellman, J. A. “Optimization of a Somatostatin Mimetic via Constrained Amino Acid and Backbone Incorporation” Bioorg. Med. Chem. Lett. 10, 2731-2733 (2000). ::doi::

 

80.      Lee, A.; Szewczyk, J. W.; Ellman, J. A. “Combinatorial Libraries for Drug Development” in “Stimulating Concepts in Chemistry” Vogtle, F.; Stoddart, J. F.; Shibasaki, M. Ed.; Wiley-VCH, Weinheim, 2000, pp. 65-78.

 

79.      Ellman, J. A. “Combinatorial Methods to Engineer Small Molecules for Functional Genomics”, in Ernst Schering Research Foundation Workshop 32, “The Role of Natural Products in Drug Discovery” Mulzer, J. and Bohlmann, R. Ed.; Springer, New York , 2000, pp. 183-204.

 

78.      Bi, X.; Lin, B. Haque, T.; Lee, C. E.; Skillman, A. G.; Kuntz, I. D.; Ellman, J. A.; Lynch, G. “Novel Cathepsin D Inhibitors Block the Formation of Hyperphosphorylated Tau Fragments in Hippocampus” J. Neurochem. 74, 1469-1477 (2000). ::doi::

 

77.      Maly, D. J.; Choong, I. C.; Ellman, J. A. “Combinatorial Target-Guided Ligand Assembly.  Identification of Potent, Sub-type Selective c-Src Inhibitors” Proc. Natl. Acad. Sci. 97, 2419-2424 (2000).

 

76.      Souers, A. J.; Ellman, J. A. “Asymmetric Synthesis of a C-3 Substituted Pipecolic Acid” J. Org. Chem. 65, 1222-1224 (2000). ::doi::

 

75.      Backes, B. J.; Harris, J. L.; Leonetti, F.; Craik, C.; Ellman, J. A. “Strategy to Prepare Positional Scanning Libraries of Fluorogenic Peptide Substrates that Incorporate Diverse P1 Substituents:  Facile and Accurate Specificity Determination of Thrombin and Plasmin” Nat. Biotechnol. 18, 187-194 (2000). ::doi::

74.      Shin, Y.; Winans, K. A.; Backes, B. J.; Kent, S. B. H.; Ellman, J. A.; Bertozzi, C. R. “Fmoc-Based Synthesis of Peptide-Thioesters: Application to the Total Chemical Synthesis of a Glycoprotein by Native Chemical Ligation” J. Am. Chem. Soc. 121, 11684-11689 (1999). ::doi::

73.      Lee, A.; Huang, L.; Ellman, J. A. “General Solid-phase Method for the Preparation of Mechanism-Based Cysteine Protease Inhibitors” J. Am. Chem. Soc. 121, 9907-9914 (1999). ::doi::

72.      Dragoli, D. R.; Ellman, J. A. “Parallel Solid-Phase Synthesis of Prostaglandin E Analogs” J. Comb. Chem. 1, 534-539 (1999). ::doi::

71.      Huang, L.; Lee, A.; Ellman, J. A. “Targeted Libraries”, in Proceedings of the 16th American Peptide Symposium, Fields, G. B.; Tam, J. P.; and Kerwin, J. F. Ed.; Kluwer Academic Publishers, Inc.: Boston, 2000, pp. 161-163.

70.      Haskell-Leuvano, C.; Souers, A. J.; Rosenquist, A., Ellman, J. A.; Cone, R. D. “Identification of Agonists at the Human Melanocortin Receptor MC1R By the Evaluation of a Library of Small Molecules Based upon the b-Turn” J. Med. Chem. 42, 4380-4387 (1999). ::doi::

69.      Ramdas, L.; Bunin, B. A.; Plunkett, M. J.; Sun, G.; Ellman, J. A.; Gallick, G.; Budde, R. J. A. “Benzodiazepine Compounds as Inhibitors of the Src Protein Tyrosine Kinase: Screening of a Combinatorial Library of 1,4-Benzodiazepines” Archives of Biochem. And Biophys. 368, 394-400 (1999). ::doi::

68.      Choong, I. C.; Ellman, J. A. “Expedient Synthesis of Alkoxylamines Using tert-Butyl Oxaziridine: The First Direct Amination of Alcohols” J. Org. Chem. 64, 6528-6529 (1999). ::doi::

67.      Borg, G.; Cogan, D. A.; Ellman, J. A. “One-Pot Asymmetric Reductive Amination of Ketones to Prepare tert-Butanesulfinyl Protected Amines” Tetrahedron Lett. 40, 6709-6712 (1999). ::doi::

66.      Backes, B. J.; Dragoli, D. R.; Ellman, J. A. “Chiral N-Acyl-tert-Butanesulfinamides:  The “Safety-Catch” Principle Applied to Diastereoselective Enolate Alkylations” J. Org. Chem. 64, 5472-5478 (1999). ::doi::

65.      Xu, R.; Greiveldinger, G.; Marenus, L. E.; Cooper, A. G.; Ellman, J. A. “Combinatorial Library Approach to the Development of Synthetic Receptors Targeting Vancomycin Resistant Bacteria” J. Am. Chem. Soc. 121, 4898-4899 (1999). ::doi::

64.      Cogan, D. A.; Liu, G.; Ellman, J. A. “Asymmetric Synthesis of Chiral Amines by Highly Diastereoselective 1,2-Additions of Organometallic Reagents to N-tert-Butanesulfinyl Imines” Tetrahedron 55, 8883-8904 (1999). ::doi::

63.      Haque, T. S.; Skillman, A. G.; Lee, C. E.; Habashita, H.; Gluzman, I. Y.; Ewing, T. J. A.; Goldberg, D. E.; Kuntz, I. D.; Ellman, J. A. “Single Digit Nanomolar, Low Molecular Weight Non-Peptide Inhibitors of Malarial Aspartyl Protease Plasmepsin II” J. Med. Chem. 42, 1428-1440 (1999). ::doi::

62.      Backes, B. J.; Ellman, J. A. “An Alkanesulfonamide “Safety-Catch” Linker for Solid-Phase Synthesis” J. Org. Chem. 64, 2322-2330 (1999). ::doi::

61.      Souers, A. J.; Schürer, Kwack, H.; Virgilio, A. A.; Ellman, J. A. “Preparation of Enantioenriched alpha-Bromo Acids with Diverse Side Chain Functionality” Synthesis, 583-585 (1999). ::doi::

60.      Liu, G.; Cogan, D. A.; Owens, T. D.; Tang, T. P.; Ellman, J. A. “The Synthesis of Enantiomerically Pure N-tert-Butanesulfinyl Imines (tert-Butanesulfinimines) by the Direct Condensation of tert-Butanesulfinamide with Aldehydes and Ketones” J. Org. Chem. 64, 1278-1284 (1999). ::doi::

59.      Souers, A. J.; Virgilio, A. A.; Rosenquist, A.; Fenuik, W. Ellman, J. A. “Identification of a Potent Heterocyclic Ligand to Somatostatin Receptor Sub-Type 5 by the Synthesis and Screening of beta-Turn Mimetic Libraries” J. Am. Chem. Soc. 121, 1817-1825 (1999). ::doi::

58.      Cogan, D. A.; Ellman, J. A. “The Asymmetric Synthesis of alpha,alpha-Dibranched Amines by the Trimethylaluminum Mediated 1,2-Addition of Organolithiums to tert-Butanesulfinyl Ketimines” J. Am. Chem. Soc. 121, 268-269 (1999). ::doi::

57.      Tang, T. P.; Ellman, J. A. “The tert-Butanesulfinyl Group: An Ideal Chiral Directing Group and Boc-Surrogate for Asymmetric  beta-Amino Acid Synthesis and Applications” J. Org. Chem. 64, 12-13 (1999). ::doi::

56.      Kim, K.; Volkman, S. K.; Ellman, J. A. “Synthesis of 3-Substituted 1,4-Benzodiazepin-2-ones” J. Braz. Chem. Soc. 9, 375-379 (1998).

55.      Lee, C. E.; Kick, E. K.; Ellman, J. A. “General Solid-Phase Synthesis Approach to Prepare Mechanism-Based Aspartyl Protease Inhibitor Libraries.  Identification of Potent Cathepsin D Inhibitors” J. Am. Chem. Soc. 120, 9735-9748 (1998). ::doi::

54.      Souers, A. J.; Virgilio, A. A.; Schürer, S. S.; Ellman, J. A.; Vanderslice, P.; Kogan, T. P. “Novel Inhibitors of alpha-4-beta-1 Integrin Receptor Interactions Through Library Synthesis and Screening” Bioorg. Med. Chem. Lett. 8, 2297-2303 (1998). ::doi::

53.      Cogan, D. A.; Liu, G.; Kim, K.; Backes, B. A.; Ellman, J. A. “Catalytic Asymmetric Oxidation of tert-Butyl Disulfide.  Synthesis of tert-Butanesulfinamides, tert-Butyl Sulfoxide, and tert-Butanesulfinimines” J. Am. Chem. Soc. 120, 8011-8019 (1998). ::doi::

52.      Ellman, J. A.; Gallop, M. A. “Combinatorial Chemistry” Curr. Opin. Chem. Biol. 2, 317-319 (1998). ::doi::

51.      Thompson, L. A.; Moore, F. L.; Moon, Y.-C.; Ellman, J. A. “Solid-Phase Synthesis of Diverse E- F- Series Prostaglandins” J. Org. Chem. 63, 2066-2067 (1998). ::doi::

50.      Woolard, F. X.; Paetsch, J.; Ellman, J. A.  “A Silicon Linker for the Direct Loading of Aromatic Compounds onto Solid Supports.  Traceless Synthesis of Pyridyl-Based Tricyclics” J. Org. Chem. 62, 6102-6103 (1997). ::doi::

49.      Liu, G.; Cogan, D. A.; Ellman, J. A. “Catalytic Asymmetric Synthesis of tert-Butanesulfinamide.  Application to the Asymmetric Synthesis of Amines” J. Am. Chem. Soc.  119, 9913-9914 (1997). ::doi::

48.      Backes, B. A.; Ellman, J. A. “Solid Support Linker Strategies” Curr. Opin. Chem. Biol. 1, 86-94 (1997). ::doi::

47.      Kick, E. K.; Roe, D. C.; Skillman, A. G.; Liu, G.; Ewing, T. J. A.; Sun, Y.; Kuntz, I. D.;  Ellman, J. A. “Structure-Based Design and Combinatorial Chemistry Yield Low Nanomolar Inhibitors of Cathepsin D” Chem. Biol.  4, 297-309 (1997). ::doi::

46.      Virgilio, A. A.; Bray, A. A.; Zhang, W.; Ellman, J. A. "Synthesis and Evaluation of a Library of Peptidomimetics Based upon the beta-Turn" Tetrahedron 53, 6635-6644 (1997). ::doi::

45.      Plunkett, M. J.; Ellman, J. A. "Germanium and Silicon Linking Strategies for Traceless Solid-Phase Synthesis" J. Org. Chem. 62, 2885-2893 (1997). ::doi::

44.      Ellman, J. Stoddard, B.; Wells, J. “Combinatorial Thinking in Chemistry and Biology” Proc. Natl. Acad. Sci., USA  94, 2779-2782 (1997).

43.      Evans, D. A.; Barrow, J. C.; Watson, P. S.; Ratz, A. M.; Dinsmore, C. J.; Evrard, D. A.; DeVries, K.; Ellman, J. A.; Rychnovsky, S. D.; Lacour, J. “Synthesis and Conformational Properties of the M(4-6)(5-7) Bicyclic Tetrapeptide Common to the Vancomycin Antibiotics” J. Am. Chem. Soc. 119, 3419-3420 (1997). ::doi::

42.      Boojamra, C. G.; Burow, K. M.; Thompson, L. A.; Ellman, J. A. "The Solid-Phase Synthesis of 1,4-Benzodiazepine-2,5-diones.  Library Preparation and Demonstration of Synthesis Generality" J. Org. Chem. 62, 1240-1257 (1997). ::doi::

41.      Plunkett, M. J.; Ellman, J. A. "Combinatorial Chemistry and New Drugs" Sci. Am. 276, 68-73 (1997).

40.      Plunkett, M. J.; Ellman, J. A. "Combinatorial Chemistry" McGraw-Hill Yearbook of Science & Technology 1997 Parker, S. P., Ed.; McGraw-Hill Book Co.: New York, New York, 1997, pp. 95-99.

39.      Bunin, B. A.; Plunkett, M. J.; Bray, A. M.; Ellman, J. A. "The Synthesis of a 1680 Compound 1,4-Benzodiazepine Library" New J. Chem. 21, 125 (1997).

38.      Choong, I. C.; Ellman, J. A. "Solid-Phase Synthesis: Application of Combinatorial Libraries" in Annu. Rep. Med. Chem. 31, 309-318 (1996). ::doi::

37.      Stevens, S. Y.; Bunin, B. A.; Plunkett, M. J.; Swanson, P. C.; Ellman, J. A.; Glick, G. D. "Non-Nucleic Acid Inhibitors of Protein-DNA Interactions Identified through Combinatorial Chemistry" J. Am. Chem. Soc. 118, 10650-10651 (1996). ::doi::

36.      Virgilio, A. A.; Schürer, S.; Ellman, J. A. "Expedient Synthesis of beta-Turn Mimetics Incorporating the i + 1, i + 2, and i + 3 Sidechains" Tetrahedron Lett. 37, 6961-6964 (1996). ::doi::

35.      Backes, B. J.; Virgilio, A. A.; Ellman, J. A. "Enhanced Activation of Kenner 's Safety-Catch Linker.  Applications to Solid-Phase Synthesis" J. Am. Chem. Soc. 118, 3055-3057 (1996). ::doi::

34.      Koh, J. S.; Ellman, J. A. "Palladium-Mediated Three-Component Coupling Strategy for the Solid-Phase Synthesis of Tropane Derivatives" J. Org. Chem. 61, 4494-4495 (1996). ::doi::

33.      Virgilio, A. A.; Ellman, J. A. "Conformationally Restricted Peptide and Peptidomimetic Libraries" in Combinatorial Chemistry and Molecular Diversity in Drug Discovery; Gordon, E. M. and Kerwin, J. F. Ed.; John Wiley & Sons, Inc.: New York, New York, 1998, pp. 133-151.

32.      Ellman, J. A. "The Solid-Phase Synthesis of Complex Small Molecules" Chimia 50, 260-261 (1996).

31.      Ellman, J. A. "Design, Synthesis, and Evaluation of Small-Molecule Libraries" Acc. Chem. Res. 29, 132-143 (1996). ::doi::

30.      Thompson, L. A.; Ellman, J. A. "Synthesis and Applications of Small Molecule Libraries" Chem. Rev. 96, 555-600 (1996). ::doi::

29.      Liu, G.; Ellman, J. A. "Combinatorial Asymmetric Catalyst Development.  General Solid-Phase Synthesis Strategy for the Preparation of 2-Pyrrolidinemethanol Ligands" J. Org. Chem. 60, 7712-7713 (1995). ::doi::

28.      Plunkett, M. J.; Ellman, J. A. "Silicon-Based Linkage Strategy for Traceless Solid-Phase Synthesis" J. Org. Chem. 60, 6006-6007 (1995). ::doi::

27.      Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. "Synthesis and Evaluation of 1,4-Benzodiazepine Libraries" Methods Enzymol. 267, 448-467 (1996). ::doi::

26.      Boojamra, C G.; Burow, K. J.; Ellman, J. A. "A General and Straightforward Method for the Solid-Phase Synthesis of 1,4-Benzodiazepine-2,5-diones" J. Org. Chem. 60, 5742-5743 (1995). ::doi::

25.      Ellman, J. A. "Synthesis and Evaluation of 1,4-Benzodiazepine Libraries" in Combinatorial Peptide and Nonpeptide Libraries; Jung, G. Ed.; VCH Verlagsgesellschaft mbH: Weinham, Germany, 1996, pp. 405-424.

24.      Ellman, J. A. "Combinatorial Organic Libraries" CHEMTRACTS: Org. Chem. 8, 1-4 (1995).

23.      Kick, E. K.; Ellman, J. A. "Expedient Method for the Solid-Phase Synthesis of Aspartic Acid Protease Inhibitors Directed toward the Generation of Libraries" J. Med. Chem. 38, 1427-1430 (1995). ::doi::

22.      Plunkett, M. J.; Ellman, J. A. "Stille Coupling in the Solid-Phase Synthesis of Structurally Diverse 1,4-Benzodiazepine Derivatives" J. Am. Chem. Soc. 117, 3306-3307 (1995). ::doi::

21.      Thompson, L. A.; Ellman, J. A. "Straightforward and General Method for Coupling Alcohols to Solid-Supports" Tetrahedron Lett. 35, 9333-9336 (1994). ::doi::

20.      Virgilio, A. A.; Ellman, J. A. "Simultaneous Solid-Phase Synthesis of beta-Turn Mimetics Incorporating Side-Chain Functionality" J. Am. Chem. Soc. 116, 11580-11581 (1994). ::doi::

19.      Backes, B. J.; Ellman, J. A. "Carbon-Carbon Bond Forming Methods on Solid Support.  Utilization of Kenner's "Safety-Catch" Linker" J. Am. Chem. Soc. 116, 11171-11172 (1994). ::doi::

18.      Bunin, B. A.; Ellman, J. A. "Increasing the Diversity of a 1,4-Benzodiazepine Library through Side-Chain Functionalization" Polym. Prepr. 35, 983, (1994).

17.      Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. "The Combinatorial Synthesis, and Chemical and Biological Evaluation of a 1,4-Benzodiazepine Library" Proc. Natl. Acad. Sci USA, 91, 4708-4712 (1994).

16.      Bunin, B. A.; Ellman, J. A. "A General and Expedient Method for the Solid-Phase Synthesis of 1,4-Benzodiazepine Derivatives" J. Am. Chem. Soc. 114, 10997-10998 (1992). ::doi:: Commentaries on the publication were reported in both Chemical and Engineering News 71, 33-34 (1993) and in the New Scientist   137, 14 (1993).

15.      Cook, S. N.; Jack, W. E.; Xiong, X.; Danley, L. E.; Ellman, J. A.; Schultz, P. G.; Noren, C. J. "Photochemically-Initiated Protein Splicing" Protein Eng. 8, 87 (1995).

14.      Cook, S. N.; Jack, W. E.; Xiong, X.; Danley, L. E.; Ellman, J. A.; Schultz, P. G.; Noren, C. J. "Photochemically-Initiated Protein Splicing" Angew. Chem., Int. Ed. Engl. 34, 1629-1630 (1995). ::doi::

13.      Mendel, D.; Ellman, J. A.; Schultz, P. G. "Probing Protein Biosynthesis with Conformationally Restricted Amino Acids" J. Am. Chem. Soc. 115, 4359-4360 (1993). ::doi::

12.      Ellman, J. A.; Volkman, B. F.; Mendel, D.; Schultz, P. G.; Wemmer, D. E. "Site-Specific Isotopic Labeling of Proteins for NMR Studies"J. Am. Chem. Soc. 114, 7959-7961 (1992). ::doi::

11.      Mendel, D.; Ellman, J. A.; Chang, Z.; Veenstra, D. L.; Kollman, P. A.; Schultz, P. G. "Probing Protein Stability with Unnatural Amino Acids" Science 256, 1798-1802 (1992). ::doi::

10.      Ellman, J. A.; Mendel, D. Schultz, P. G. "Site-Specific Incorporation of Novel Backbone Structures into Proteins" Science 255, 197-200 (1992). ::doi::

9.      Ellman, J. A.; Mendel, D.; Noren, C. J.; Anthony-Cahill, S. J.; Schultz, P. G. "A Biosynthetic Method for Introducing Unnatural Amino Acids Site-Specifically into Proteins" Methods Enzymol.  202, 301-336 (1991). ::doi::

8.      Mendel, D.; Ellman J. A.; Schultz, P. G. "Construction of a Light-Activated Protein by Unnatural Amino Acid Mutagenesis"  J. Am. Chem. Soc. 113, 2758-2760 (1991). ::doi::

7.      Robertson, S. A.; Ellman, J. A.; Schultz, P. G. "A General and Efficient Route for Chemical Aminoacylation of Transfer RNAs" J. Am. Chem. Soc. 113, 2722-2729 (1991). ::doi::

6.      Evans, D. A.; Britton, T. C.; Ellman, J. A.; Dorow, R. L. "The Asymmetric Synthesis of alpha-Amino Acids.  Electrophilic Azidation of Chiral Imide Enolates, a Practical Approach to the Synthesis of (R)- and (S)- alpha-Azido Carboxylic Acids" J. Am. Chem. Soc. 112, 4011-4030 (1990). ::doi::

5.      Evans, D. A.; Ellman, J. A.; DeVries, K. M. "The Oxidative Macrocyclization of Phenolic Peptides.  A Biomimetic Approach to the Synthesis of the Vancomycin Family of Antibiotics" J. Am. Chem. Soc. 111, 8912-8914 (1989). ::doi::

4.      Evans, D. A.; Ellman, J. A. "The Total Synthesis of the Isodityrosine-Derived Cyclic Tripeptides OF4949-III and K-13.  Determination of the Absolute Configuration of K-13" J. Am. Chem. Soc. 111, 1063-1072 (1989). ::doi::

3.      Evans, D. A.; Ellman, J. A.; Dorow, R. L. "Asymmetric Halogenation of Chiral Imide Enolates.  A General Approach to the Synthesis of Enantiomerically Pure alpha-Amino Acids" Tetrahedron Lett. 28, 1123-1126 (1987). ::doi::

2.      Evans, D. A; Britton, T. C.; Ellman, J. A. "Contrasteric Carboximide Hydrolysis with Lithium Hydroperoxide" Tetrahedron Lett. 28, 6141-6144 (1987). ::doi::

1.      Evans, D. A.; Weber, A. E.; Britton, T. C.; Ellman, J. A.; Sjogren, E. B. "Asymmetric Synthesis of Amino Acids" in Peptides: Chemistry And Biology; Tenth American Peptide Symposium; Marshall, G. R. (Ed.); Escom Science Publishers B.V.: Leiden, Netherlands. Illus. 143-148 (1988).

 

 

Patents

 

1.            Harris, J. L.; Backes, B. J.; Ellman, J. A.; Craik, C. S. “Profiling of protease specificity using combinatorial fluorogenic substrate libraries” U.S. (2004) US patent number 6,680,178.

 

2.            Ellman, J. A.; Choong, I. “Pharmacophore Recombination for the Identification of Small Molecule Drug Lead Compounds” U.S. (2002), Patent No. 6,344,334.

 

3.            Ellman, J. A.; Choong, I. “Pharmacophore Recombination for the Identification of Small Molecule Drug Lead Compounds” U.S. (2002), Patent No. 6,344,330.

 

4.            Kim, J. M.; Ellman, J. A.; Goldberg, D.  “Preparation of 4-amino-1-benzylpiperidines as antimalarials” PCT Int. Appl. (2001), WO  0114331 A2  2001030.

 

5.            Kick, E. K.; Ellman, J. A.; Kuntz, I. D.; Lee, C. E.; Liu, G.; Roe, D. C.; Skillman, A. G. “Nanomolar, Non-Peptide Inhibitors of Cathepsin D U. S. (2000), Patent No. 6,150,416.

 

6.            Ellman, J. A.; Lynch, G.; Kuntz, I. D.; Bi, X.; Lee, C. E.; Skillman, A. G.; Haque, T.  “Methods for treating neurodegenerative disorders using aspartyl protease inhibitors”  PCT Int. Appl.  (2000), WO  0056335 A1 20000928.

 

7.            Ellman, J. A.; Choong, I. “Pharmacophore Recombination for the Identification of Small Molecule Drug Lead Compounds” PCT Int. Appl. (1999), WO 9949314 A1 19990930.

 

8.            Budde, R, J. A.; Ellman, J. A.; Levin, V. A.; Gallick, G. E.; Newman, R. A.; “Preparation of Benzodiazepinones as Protein Tyrosine Kinase Inhibitors” PCT Int. Appl. (1999), WO 9919306 A2 19990422.

 

9.            Ellman, J. A.  “Solid phase and combinatorial synthesis of benzodiazepines on a solid support” U.S.  (1996), Cont.-in-part of U.S. 5,288,514.

 

10.        Ellman, J. A. "Solid-Phase and Combinatorial Synthesis of Benzodiazepine Compounds on a Solid Support" U.S. (1994), Patent No. 5,288,514.