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Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6- methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.
Chu XJ, DePinto W, Bartkovitz D, So SS, Vu BT, Packman K, Lukacs C, Ding Q, Jiang N, Wang K, Goelzer P, Yin X, Smith MA, Higgins BX, Chen Y, Xiang Q, Moliterni J, Kaplan G, Graves B, Lovey A, Fotouhi N. Chu XJ, et al. Among authors: chen y. J Med Chem. 2006 Nov 2;49(22):6549-60. doi: 10.1021/jm0606138. J Med Chem. 2006. PMID: 17064073
3,5,6-Trisubstituted naphthostyrils as CDK2 inhibitors.
Liu JJ, Dermatakis A, Lukacs C, Konzelmann F, Chen Y, Kammlott U, Depinto W, Yang H, Yin X, Chen Y, Schutt A, Simcox ME, Luk KC. Liu JJ, et al. Among authors: chen y. Bioorg Med Chem Lett. 2003 Aug 4;13(15):2465-8. doi: 10.1016/s0960-894x(03)00488-8. Bioorg Med Chem Lett. 2003. PMID: 12852944
In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials.
DePinto W, Chu XJ, Yin X, Smith M, Packman K, Goelzer P, Lovey A, Chen Y, Qian H, Hamid R, Xiang Q, Tovar C, Blain R, Nevins T, Higgins B, Luistro L, Kolinsky K, Felix B, Hussain S, Heimbrook D. DePinto W, et al. Among authors: chen y. Mol Cancer Ther. 2006 Nov;5(11):2644-58. doi: 10.1158/1535-7163.MCT-06-0355. Mol Cancer Ther. 2006. PMID: 17121911
Identification of novel, potent and selective inhibitors of Polo-like kinase 1.
Chen S, Bartkovitz D, Cai J, Chen Y, Chen Z, Chu XJ, Le K, Le NT, Luk KC, Mischke S, Naderi-Oboodi G, Boylan JF, Nevins T, Qing W, Chen Y, Wovkulich PM. Chen S, et al. Among authors: chen z, chen y. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1247-50. doi: 10.1016/j.bmcl.2011.11.052. Epub 2011 Dec 1. Bioorg Med Chem Lett. 2012. PMID: 22172702
Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.
McDermott LA, Higgins B, Simcox M, Luk KC, Nevins T, Kolinsky K, Smith M, Yang H, Li JK, Chen Y, Ke J, Mallalieu N, Egan T, Kolis S, Railkar A, Gerber L, Liu JJ, Konzelmann F, Zhang Z, Flynn T, Morales O, Chen Y. McDermott LA, et al. Among authors: chen y. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3. doi: 10.1016/j.bmcl.2005.12.092. Epub 2006 Feb 3. Bioorg Med Chem Lett. 2006. PMID: 16460940
Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.
Chen S, Chen L, Le NT, Zhao C, Sidduri A, Lou JP, Michoud C, Portland L, Jackson N, Liu JJ, Konzelmann F, Chi F, Tovar C, Xiang Q, Chen Y, Wen Y, Vassilev LT. Chen S, et al. Among authors: chen l, chen y. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2134-8. doi: 10.1016/j.bmcl.2007.01.081. Epub 2007 Jan 31. Bioorg Med Chem Lett. 2007. PMID: 17303421
Metal impurities cause false positives in high-throughput screening campaigns.
Hermann JC, Chen Y, Wartchow C, Menke J, Gao L, Gleason SK, Haynes NE, Scott N, Petersen A, Gabriel S, Vu B, George KM, Narayanan A, Li SH, Qian H, Beatini N, Niu L, Gan QF. Hermann JC, et al. Among authors: chen y. ACS Med Chem Lett. 2012 Dec 12;4(2):197-200. doi: 10.1021/ml3003296. eCollection 2013 Feb 14. ACS Med Chem Lett. 2012. PMID: 24900642 Free PMC article.
Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes.
Qian Y, Wertheimer SJ, Ahmad M, Cheung AW, Firooznia F, Hamilton MM, Hayden S, Li S, Marcopulos N, McDermott L, Tan J, Yun W, Guo L, Pamidimukkala A, Chen Y, Huang KS, Ramsey GB, Whittard T, Conde-Knape K, Taub R, Rondinone CM, Tilley J, Bolin D. Qian Y, et al. Among authors: chen y. J Med Chem. 2011 Apr 14;54(7):2433-46. doi: 10.1021/jm101580m. Epub 2011 Mar 17. J Med Chem. 2011. PMID: 21413799
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