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Discovery of N-[2-[2-[[3-methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4- morpholineacetamide as a novel and potent inhibitor of inosine monophosphate dehydrogenase with excellent in vivo activity.
Dhar TG, Shen Z, Guo J, Liu C, Watterson SH, Gu HH, Pitts WJ, Fleener CA, Rouleau KA, Sherbina NZ, McIntyre KW, Shuster DJ, Witmer MR, Tredup JA, Chen BC, Zhao R, Bednarz MS, Cheney DL, MacMaster JF, Miller LM, Berry KK, Harper TW, Barrish JC, Hollenbaugh DL, Iwanowicz EJ. Dhar TG, et al. Among authors: zhao r. J Med Chem. 2002 May 23;45(11):2127-30. doi: 10.1021/jm0105777. J Med Chem. 2002. PMID: 12014950
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
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
C-3 Amido-indole cannabinoid receptor modulators.
Hynes J Jr, Leftheris K, Wu H, Pandit C, Chen P, Norris DJ, Chen BC, Zhao R, Kiener PA, Chen X, Turk LA, Patil-Koota V, Gillooly KM, Shuster DJ, McIntyre KW. Hynes J Jr, et al. Among authors: zhao r. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2399-402. doi: 10.1016/s0960-894x(02)00466-3. Bioorg Med Chem Lett. 2002. PMID: 12161142
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 Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).
Watterson SH, Liu Q, Beaudoin Bertrand M, Batt DG, Li L, Pattoli MA, Skala S, Cheng L, Obermeier MT, Moore R, Yang Z, Vickery R, Elzinga PA, Discenza L, D'Arienzo C, Gillooly KM, Taylor TL, Pulicicchio C, Zhang Y, Heimrich E, McIntyre KW, Ruan Q, Westhouse RA, Catlett IM, Zheng N, Chaudhry C, Dai J, Galella MA, Tebben AJ, Pokross M, Li J, Zhao R, Smith D, Rampulla R, Allentoff A, Wallace MA, Mathur A, Salter-Cid L, Macor JE, Carter PH, Fura A, Burke JR, Tino JA. Watterson SH, et al. Among authors: zhao r. J Med Chem. 2019 Apr 11;62(7):3228-3250. doi: 10.1021/acs.jmedchem.9b00167. Epub 2019 Mar 29. J Med Chem. 2019. PMID: 30893553
(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
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