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Page 1
N-Aryl-gamma-lactams as integrin alphavbeta3 antagonists.
Xi N, Arvedson S, Eisenberg S, Han N, Handley M, Huang L, Huang Q, Kiselyov A, Liu Q, Lu Y, Nunez G, Osslund T, Powers D, Tasker AS, Wang L, Xiang T, Xu S, Zhang J, Zhu J, Kendall R, Dominguez C. Xi N, et al. Among authors: zhang j. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2905-9. doi: 10.1016/j.bmcl.2004.03.033. Bioorg Med Chem Lett. 2004. PMID: 15125957
Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors.
Zhong W, Liu H, Kaller MR, Henley C, Magal E, Nguyen T, Osslund TD, Powers D, Rzasa RM, Wang HL, Wang W, Xiong X, Zhang J, Norman MH. Zhong W, et al. Among authors: zhang j. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5384-9. doi: 10.1016/j.bmcl.2007.07.045. Epub 2007 Aug 6. Bioorg Med Chem Lett. 2007. PMID: 17709247
The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors.
Yuan C, St Jean DJ Jr, Liu Q, Cai L, Li A, Han N, Moniz G, Askew B, Hungate RW, Johansson L, Tedenborg L, Pyring D, Williams M, Hale C, Chen M, Cupples R, Zhang J, Jordan S, Bartberger MD, Sun Y, Emery M, Wang M, Fotsch C. Yuan C, et al. Among authors: zhang j. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6056-61. doi: 10.1016/j.bmcl.2007.09.070. Epub 2007 Sep 25. Bioorg Med Chem Lett. 2007. PMID: 17919905
Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.
Fotsch C, Bartberger MD, Bercot EA, Chen M, Cupples R, Emery M, Fretland J, Guram A, Hale C, Han N, Hickman D, Hungate RW, Hayashi M, Komorowski R, Liu Q, Matsumoto G, St Jean DJ Jr, Ursu S, Véniant M, Xu G, Ye Q, Yuan C, Zhang J, Zhang X, Tu H, Wang M. Fotsch C, et al. Among authors: zhang j, zhang x. J Med Chem. 2008 Dec 25;51(24):7953-67. doi: 10.1021/jm801073z. J Med Chem. 2008. PMID: 19053753
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles.
St Jean DJ Jr, Ashton KS, Bartberger MD, Chen J, Chmait S, Cupples R, Galbreath E, Helmering J, Hong FT, Jordan SR, Liu L, Kunz RK, Michelsen K, Nishimura N, Pennington LD, Poon SF, Reid D, Sivits G, Stec MM, Tadesse S, Tamayo N, Van G, Yang KC, Zhang J, Norman MH, Fotsch C, Lloyd DJ, Hale C. St Jean DJ Jr, et al. Among authors: zhang j. J Med Chem. 2014 Jan 23;57(2):325-38. doi: 10.1021/jm4016747. Epub 2014 Jan 9. J Med Chem. 2014. PMID: 24405213
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept.
Ashton KS, Andrews KL, Bryan MC, Chen J, Chen K, Chen M, Chmait S, Croghan M, Cupples R, Fotsch C, Helmering J, Jordan SR, Kurzeja RJ, Michelsen K, Pennington LD, Poon SF, Sivits G, Van G, Vonderfecht SL, Wahl RC, Zhang J, Lloyd DJ, Hale C, St Jean DJ Jr. Ashton KS, et al. Among authors: zhang j. J Med Chem. 2014 Jan 23;57(2):309-24. doi: 10.1021/jm4016735. Epub 2014 Jan 9. J Med Chem. 2014. PMID: 24405172
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
Véniant MM, Hale C, Hungate RW, Gahm K, Emery MG, Jona J, Joseph S, Adams J, Hague A, Moniz G, Zhang J, Bartberger MD, Li V, Syed R, Jordan S, Komorowski R, Chen MM, Cupples R, Kim KW, St Jean DJ Jr, Johansson L, Henriksson MA, Williams M, Vallgårda J, Fotsch C, Wang M. Véniant MM, et al. Among authors: zhang j. J Med Chem. 2010 Jun 10;53(11):4481-7. doi: 10.1021/jm100242d. J Med Chem. 2010. PMID: 20465278
Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ*S-X) Interaction for Conformational Constraint.
Pennington LD, Bartberger MD, Croghan MD, Andrews KL, Ashton KS, Bourbeau MP, Chen J, Chmait S, Cupples R, Fotsch C, Helmering J, Hong FT, Hungate RW, Jordan SR, Kong K, Liu L, Michelsen K, Moyer C, Nishimura N, Norman MH, Reichelt A, Siegmund AC, Sivits G, Tadesse S, Tegley CM, Van G, Yang KC, Yao G, Zhang J, Lloyd DJ, Hale C, St Jean DJ Jr. Pennington LD, et al. Among authors: zhang j. J Med Chem. 2015 Dec 24;58(24):9663-79. doi: 10.1021/acs.jmedchem.5b01367. Epub 2015 Dec 1. J Med Chem. 2015. PMID: 26551034 Free article.
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