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10,438 results

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Page 1
Use of a Conformational-Switching Mechanism to Modulate Exposed Polarity: Discovery of CCR2 Antagonist BMS-741672.
Yang MG, Xiao Z, Cherney RJ, Tebben AJ, Batt DG, Brown GD, Chen J, Cvijic ME, Dabros M, Duncia JV, Galella M, Gardner DS, Khandelwal P, Ko SS, Malley MF, Mo R, Pang J, Rose AV, Santella JB 3rd, Shi H, Srivastava A, Traeger SC, Wang B, Xu S, Zhao R, Barrish JC, Mandlekar S, Zhao Q, Carter PH. Yang MG, et al. Among authors: zhao r, zhao q. ACS Med Chem Lett. 2019 Jan 16;10(3):300-305. doi: 10.1021/acsmedchemlett.8b00439. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891130 Free PMC article.
N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent.
Misra RN, Xiao HY, Kim KS, Lu S, Han WC, Barbosa SA, Hunt JT, Rawlins DB, Shan W, Ahmed SZ, Qian L, Chen BC, Zhao R, Bednarz MS, Kellar KA, Mulheron JG, Batorsky R, Roongta U, Kamath A, Marathe P, Ranadive SA, Sack JS, Tokarski JS, Pavletich NP, Lee FY, Webster KR, Kimball SD. Misra RN, et al. Among authors: zhao r. J Med Chem. 2004 Mar 25;47(7):1719-28. doi: 10.1021/jm0305568. J Med Chem. 2004. PMID: 15027863
Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.
Chen P, Norris D, Das J, Spergel SH, Wityak J, Leith L, Zhao R, Chen BC, Pitt S, Pang S, Shen DR, Zhang R, De Fex HF, Doweyko AM, McIntyre KW, Shuster DJ, Behnia K, Schieven GL, Barrish JC. Chen P, et al. Among authors: zhao r. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6061-6. doi: 10.1016/j.bmcl.2004.09.093. Bioorg Med Chem Lett. 2004. PMID: 15546730
(3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(methyl(1-methyl-1h-1,2,4-triazol-5-yl)amino)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic acid (BMS-644950): a rationally designed orally efficacious 3-hydroxy-3-methylglutaryl coenzyme-a reductase inhibitor with reduced myotoxicity potential.
Ahmad S, Madsen CS, Stein PD, Janovitz E, Huang C, Ngu K, Bisaha S, Kennedy LJ, Chen BC, Zhao R, Sitkoff D, Monshizadegan H, Yin X, Ryan CS, Zhang R, Giancarli M, Bird E, Chang M, Chen X, Setters R, Search D, Zhuang S, Nguyen-Tran V, Cuff CA, Harrity T, Darienzo CJ, Li T, Reeves RA, Blanar MA, Barrish JC, Zahler R, Robl JA. Ahmad S, et al. Among authors: zhao r. J Med Chem. 2008 May 8;51(9):2722-33. doi: 10.1021/jm800001n. Epub 2008 Apr 15. J Med Chem. 2008. PMID: 18412317
Identification of a nonbasic melanin hormone receptor 1 antagonist as an antiobesity clinical candidate.
Washburn WN, Manfredi M, Devasthale P, Zhao G, Ahmad S, Hernandez A, Robl JA, Wang W, Mignone J, Wang Z, Ngu K, Pelleymounter MA, Longhi D, Zhao R, Wang B, Huang N, Flynn N, Azzara AV, Barrish JC, Rohrbach K, Devenny JJ, Rooney S, Thomas M, Glick S, Godonis HE, Harvey SJ, Cullen MJ, Zhang H, Caporuscio C, Stetsko P, Grubb M, Maxwell BD, Yang H, Apedo A, Gemzik B, Janovitz EB, Huang C, Zhang L, Freeden C, Murphy BJ. Washburn WN, et al. Among authors: zhao g, zhao r. J Med Chem. 2014 Sep 25;57(18):7509-22. doi: 10.1021/jm500026w. Epub 2014 Sep 9. J Med Chem. 2014. PMID: 25165888
Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor.
Liu C, Lin J, Hynes J, Wu H, Wrobleski ST, Lin S, Dhar TG, Vrudhula VM, Sun JH, Chao S, Zhao R, Wang B, Chen BC, Everlof G, Gesenberg C, Zhang H, Marathe PH, McIntyre KW, Taylor TL, Gillooly K, Shuster DJ, McKinnon M, Dodd JH, Barrish JC, Schieven GL, Leftheris K. Liu C, et al. Among authors: zhao r. J Med Chem. 2015 Oct 8;58(19):7775-84. doi: 10.1021/acs.jmedchem.5b00839. Epub 2015 Sep 22. J Med Chem. 2015. PMID: 26359680
Design and Synthesis of a New Series of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes as α7 Nicotinic Receptor Agonists. 1. Development of Pharmacophore and Early Structure-Activity Relationship.
Cook J, Zusi FC, McDonald IM, King D, Hill MD, Iwuagwu C, Mate RA, Fang H, Zhao R, Wang B, Cutrone J, Ma B, Gao Q, Knox RJ, Matchett M, Gallagher L, Ferrante M, Post-Munson D, Molski T, Easton A, Miller R, Jones K, Digavalli S, Healy F, Lentz K, Benitex Y, Clarke W, Natale J, Siuciak JA, Lodge N, Zaczek R, Denton R, Morgan D, Bristow LJ, Macor JE, Olson RE. Cook J, et al. Among authors: zhao r. J Med Chem. 2016 Dec 22;59(24):11171-11181. doi: 10.1021/acs.jmedchem.6b01506. Epub 2016 Dec 13. J Med Chem. 2016. PMID: 27958732
BMS-933043, a Selective α7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia.
King D, Iwuagwu C, Cook J, McDonald IM, Mate R, Zusi FC, Hill MD, Fang H, Zhao R, Wang B, Easton AE, Miller R, Post-Munson D, Knox RJ, Gallagher L, Westphal R, Molski T, Fan J, Clarke W, Benitex Y, Lentz KA, Denton R, Morgan D, Zaczek R, Lodge NJ, Bristow LJ, Macor JE, Olson RE. King D, et al. Among authors: zhao r. ACS Med Chem Lett. 2017 Feb 8;8(3):366-371. doi: 10.1021/acsmedchemlett.7b00032. eCollection 2017 Mar 9. ACS Med Chem Lett. 2017. PMID: 28337332 Free PMC article.
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