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Robert Owen Hughes - Publications

Affiliations: 
2002 Scripps Research Institute, La Jolla, La Jolla, CA, United States 
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30 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2019 Schnute ME, Benoit SE, Buchler IP, Caspers N, Grapperhaus ML, Han S, Hotchandani R, Huang N, Hughes RO, Juba BM, Kim KH, Liu E, McCarthy E, Messing D, Miyashiro JS, et al. Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning. Acs Medicinal Chemistry Letters. 10: 80-85. PMID 30655951 DOI: 10.1021/Acsmedchemlett.8B00461  0.304
2017 Li X, Anderson M, Collin D, Muegge I, Wan J, Brennan D, Kugler S, Terenzio D, Kennedy C, Lin S, Labadia ME, Cook B, Hughes R, Farrow NA. Structural studies unravel the active conformation of apo RORγt nuclear receptor and a common inverse agonism of two diverse classes of RORγt inhibitors. The Journal of Biological Chemistry. PMID 28546429 DOI: 10.1074/Jbc.M117.789024  0.314
2011 Xue CB, Wang A, Han Q, Zhang Y, Cao G, Feng H, Huang T, Zheng C, Xia M, Zhang K, Kong L, Glenn J, Anand R, Meloni D, Robinson DJ, ... ... Hughes RO, et al. Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist. Acs Medicinal Chemistry Letters. 2: 913-8. PMID 24900280 DOI: 10.1021/Ml200199C  0.37
2011 Hughes RO, Maddux T, Joseph Rogier D, Lu S, Walker JK, Jon Jacobsen E, Rumsey JM, Zheng Y, Macinnes A, Bond BR, Han S. Investigation of the pyrazinones as PDE5 inhibitors: evaluation of regioisomeric projections into the solvent region. Bioorganic & Medicinal Chemistry Letters. 21: 6348-52. PMID 21955943 DOI: 10.1016/J.Bmcl.2011.08.106  0.35
2011 Trujillo JI, Huang W, Hughes RO, Rogier DJ, Turner SR, Devraj R, Morton PA, Xue CB, Chao G, Covington MB, Newton RC, Metcalf B. Design and synthesis of novel CCR2 antagonists: investigation of non-aryl/heteroaryl binding motifs. Bioorganic & Medicinal Chemistry Letters. 21: 1827-31. PMID 21316220 DOI: 10.1016/J.Bmcl.2011.01.052  0.39
2011 Zheng C, Cao G, Xia M, Feng H, Glenn J, Anand R, Zhang K, Huang T, Wang A, Kong L, Li M, Galya L, Hughes RO, Devraj R, Morton PA, et al. Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist. Bioorganic & Medicinal Chemistry Letters. 21: 1442-6. PMID 21295478 DOI: 10.1016/J.Bmcl.2011.01.015  0.346
2010 Tollefson MB, Acker BA, Jacobsen EJ, Hughes RO, Walker JK, Fox DN, Palmer MJ, Freeman SK, Yu Y, Bond BR. 1-(2-Ethoxyethyl)-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors. Bioorganic & Medicinal Chemistry Letters. 20: 3120-4. PMID 20443228 DOI: 10.1016/J.Bmcl.2010.03.111  0.323
2010 Tollefson MB, Acker BA, Jacobsen EJ, Hughes RO, Walker JK, Fox DN, Palmer MJ, Freeman SK, Yu Y, Bond BR. 1-(2-(2,2,2-trifluoroethoxy)ethyl-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors. Bioorganic & Medicinal Chemistry Letters. 20: 3125-8. PMID 20400309 DOI: 10.1016/J.Bmcl.2010.03.106  0.352
2010 Hughes RO, Rogier DJ, Jacobsen EJ, Walker JK, Macinnes A, Bond BR, Zhang LL, Yu Y, Zheng Y, Rumsey JM, Walgren JL, Curtiss SW, Fobian YM, Heasley SE, Cubbage JW, et al. Design, synthesis, and biological evaluation of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one, a potent, orally active, brain penetrant inhibitor of phosphodiesterase 5 (PDE5). Journal of Medicinal Chemistry. 53: 2656-60. PMID 20196613 DOI: 10.1021/Jm901781Q  0.395
2009 Hughes RO, Walker JK, Joseph Rogier D, Heasley SE, Blevis-Bal RM, Benson AG, Jon Jacobsen E, Cubbage JW, Fobian YM, Owen DR, Freskos JN, Molyneaux JM, Brown DL, Acker BA, Maddux TM, et al. Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: Discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one Bioorganic and Medicinal Chemistry Letters. 19: 5209-5213. PMID 19631533 DOI: 10.1016/J.Bmcl.2009.07.019  0.337
2009 Owen DR, Walker JK, Jon Jacobsen E, Freskos JN, Hughes RO, Brown DL, Bell AS, Brown DG, Phillips C, Mischke BV, Molyneaux JM, Fobian YM, Heasley SE, Moon JB, Stallings WC, et al. Identification, synthesis and SAR of amino substituted pyrido[3,2b]pyrazinones as potent and selective PDE5 inhibitors. Bioorganic & Medicinal Chemistry Letters. 19: 4088-91. PMID 19540112 DOI: 10.1016/J.Bmcl.2009.06.012  0.387
2009 Hughes RO, Walker JK, Cubbage JW, Fobian YM, Rogier DJ, Heasley SE, Blevis-Bal RM, Benson AG, Owen DR, Jacobsen EJ, Freskos JN, Molyneaux JM, Brown DL, Stallings WC, Acker BA, et al. Investigation of aminopyridiopyrazinones as PDE5 inhibitors: Evaluation of modifications to the central ring system. Bioorganic & Medicinal Chemistry Letters. 19: 4092-6. PMID 19539468 DOI: 10.1016/J.Bmcl.2009.06.004  0.314
2003 Nicolaou KC, Evans RM, Roecker AJ, Hughes R, Downes M, Pfefferkorn JA. Discovery and optimization of non-steroidal FXR agonists from natural product-like libraries. Organic & Biomolecular Chemistry. 1: 908-20. PMID 12929628 DOI: 10.1039/B300525A  0.763
2003 Downes M, Verdecia MA, Roecker AJ, Hughes R, Hogenesch JB, Kast-Woelbern HR, Bowman ME, Ferrer JL, Anisfeld AM, Edwards PA, Rosenfeld JM, Alvarez JG, Noel JP, Nicolaou KC, Evans RM. A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR. Molecular Cell. 11: 1079-92. PMID 12718892 DOI: 10.1016/S1097-2765(03)00104-7  0.682
2003 Nicolaou KC, Roecker AJ, Hughes R, van Summeren R, Pfefferkorn JA, Winssinger N. Novel strategies for the solid phase synthesis of substituted indolines and indoles. Bioorganic & Medicinal Chemistry. 11: 465-76. PMID 12517442 DOI: 10.1016/S0968-0896(02)00386-3  0.736
2002 Nicholas GM, Eckman LL, Ray S, Hughes RO, Pfefferkorn JA, Barluenga S, Nicolaou KC, Bewley CA. Bromotyrosine-derived natural and synthetic products as inhibitors of mycothiol-S-conjugate amidase. Bioorganic & Medicinal Chemistry Letters. 12: 2487-90. PMID 12161164 DOI: 10.1016/S0960-894X(02)00385-2  0.736
2001 Nicolaou KC, Hughes R, Pfefferkorn JA, Barluenga S. Optimization and mechanistic studies of psammaplin A type antibacterial agents active against methicillin-resistant Staphylococcus aureus (MRSA). Chemistry (Weinheim An Der Bergstrasse, Germany). 7: 4296-310. PMID 11686610 DOI: 10.1002/1521-3765(20011001)7:19<4296::Aid-Chem4296>3.0.Co;2-2  0.764
2001 Nicolaou KC, Hughes R, Pfefferkorn JA, Barluenga S, Roecker AJ. Combinatorial synthesis through disulfide exchange: discovery of potent psammaplin A type antibacterial agents active against methicillin-resistant Staphylococcus aureus (MRSA). Chemistry (Weinheim An Der Bergstrasse, Germany). 7: 4280-95. PMID 11686609 DOI: 10.1002/1521-3765(20011001)7:19<4280::Aid-Chem4280>3.0.Co;2-3  0.741
2001 Nicolaou KC, Hughes R, Cho SY, Winssinger N, Labischinski H, Endermann R. Synthesis and biological evaluation of vancomycin dimers with potent activity against vancomycin-resistant bacteria: target-accelerated combinatorial synthesis. Chemistry (Weinheim An Der Bergstrasse, Germany). 7: 3824-43. PMID 11575783 DOI: 10.1002/1521-3765(20010903)7:17<3824::Aid-Chem3824>3.0.Co;2-1  0.692
2001 Nicolaou KC, Cho SY, Hughes R, Winssinger N, Smethurst C, Labischinski H, Endermann R. Solid- and solution-phase synthesis of vancomycin and vancomycin analogues with activity against vancomycin-resistant bacteria. Chemistry (Weinheim An Der Bergstrasse, Germany). 7: 3798-823. PMID 11575782 DOI: 10.1002/1521-3765(20010903)7:17<3798::Aid-Chem3798>3.0.Co;2-6  0.652
2000 Nicolaou KC, Hughes R, Cho SY, Winssinger N, Smethurst C, Labischinski H, Endermann R. Target-Accelerated Combinatorial Synthesis and Discovery of Highly Potent Antibiotics Effective Against Vancomycin-Resistant Bacteria. Angewandte Chemie (International Ed. in English). 39: 3823-3828. PMID 29711708 DOI: 10.1002/1521-3773(20001103)39:21<3823::Aid-Anie3823>3.0.Co;2-3  0.631
2000 Nicolaou KC, Winssinger N, Hughes R, Smethurst C, Cho SY. New Selenium-Based Safety-Catch Linkers: Solid-Phase Semisynthesis of Vancomycin We thank Drs. D. H. Huang and G. Siuzdak for NMR spectroscopic and mass spectrometric assistance, respectively. This work was financially supported by the National Institutes of Health (USA), The Skaggs Institute for Chemical Biology, a fellowship from the George Hewitt Foundation (N. W.), and grants from Schering Plough, Pfizer, Glaxo, Merck, Hoffmann-La Roche, DuPont, and Abbott Laboratories. Angewandte Chemie (International Ed. in English). 39: 1084-1088. PMID 10760929 DOI: 10.1002/(Sici)1521-3773(20000317)39:6<1084::Aid-Anie1084>3.0.Co;2-O  0.615
1999 Nicolaou KC, Mitchell HJ, Jain NF, Winssinger N, Hughes R, Bando T. Total Synthesis of Vancomycin Angewandte Chemie International Edition. 38: 240-244. DOI: 10.1002/(Sici)1521-3773(19990115)38:1/2<240::Aid-Anie240>3.0.Co;2-5  0.717
1999 Nicolaou KC, Mitchell HJ, Jain NF, Bando T, Hughes R, Winssinger N, Natarajan S, Koumbis AE. Total Synthesis of Vancomycin—Part 4: Attachment of the Sugar Moieties and Completion of the Synthesis Chemistry - a European Journal. 5: 2648-2667. DOI: 10.1002/(Sici)1521-3765(19990903)5:9<2648::Aid-Chem2648>3.0.Co;2-Q  0.729
1999 Nicolaou KC, Koumbis AE, Takayanagi M, Natarajan S, Jain NF, Bando T, Li H, Hughes R. Total Synthesis Of Vancomycin. Part 3 : Synthesis Of The Aglycon Chemistry: a European Journal. 5: 2622-2647. DOI: 10.1002/(Sici)1521-3765(19990903)5:9<2622::Aid-Chem2622>3.0.Co;2-T  0.539
1999 Nicolaou KC, Boddy CNC, Li H, Koumbis AE, Hughes R, Natarajan S, Jain NF, Ramanjulu JM, Bräse S, Solomon ME. Total Synthesis of Vancomycin—Part 2: Retrosynthetic Analysis, Synthesis of Amino Acid Building Blocks and Strategy Evaluations Chemistry - a European Journal. 5: 2602-2621. DOI: 10.1002/(Sici)1521-3765(19990903)5:9<2602::Aid-Chem2602>3.0.Co;2-X  0.613
1999 Nicolaou KC, Mitchell HJ, Jain NF, Winssinger N, Hughes R, Bando T. Totalsynthese von Vancomycin Angewandte Chemie. 111: 253-255. DOI: 10.1002/(Sici)1521-3757(19990115)111:1/2<253::Aid-Ange253>3.0.Co;2-V  0.671
1998 Nicolaou KC, Jain NF, Natarajan S, Hughes R, Solomon ME, Li H, Ramanjulu JM, Takayanagi M, Koumbis AE, Bando T. Total Synthesis of Vancomycin Aglycon-Part 2: Synthesis of Amino Acids 1-3 and Construction of the AB-COD-DOE Ring Skeleton. Angewandte Chemie (International Ed. in English). 37: 2714-2716. PMID 29711613 DOI: 10.1002/(Sici)1521-3773(19981016)37:19<2714::Aid-Anie2714>3.0.Co;2-#  0.598
1998 Nicolaou KC, Natarajan S, Li H, Jain NF, Hughes R, Solomon ME, Ramanjulu JM, Boddy CNC, Takayanagi M. Total Synthesis of Vancomycin Aglycon-Part 1: Synthesis of Amino Acids 4-7 and Construction of the AB-COD Ring Skeleton. Angewandte Chemie (International Ed. in English). 37: 2708-2714. PMID 29711605 DOI: 10.1002/(SICI)1521-3773(19981016)37:19<2708::AID-ANIE2708>3.0.CO;2-E  0.547
1998 Nicolaou KC, Jain NF, Natarajan S, Hughes R, Solomon ME, Li H, Ramanjulu JM, Takayanagi M, Koumbis AE, Bando T. Totalsynthese des Vancomycin‐Aglycons – Teil 1: Synthese der Aminosäuren 4–7 und Aufbau des AB‐COD‐Ringgerüsts Angewandte Chemie. 110: 2872-2878. DOI: 10.1002/(Sici)1521-3757(19981002)110:19<2872::Aid-Ange2872>3.0.Co;2-0  0.438
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