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. 2009 Sep 1;19(17):4916-9.
doi: 10.1016/j.bmcl.2009.07.100. Epub 2009 Jul 23.

2-Amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2',3':4,5]thieno[2,3-b]pyridine derivatives as selective progesterone receptor agonists

Yonghui Wang  1 , Chaya Duraiswami, Kevin P Madauss, Thuy B Tran, Shawn P Williams, Su-Jun Deng, Todd L Graybill, Marlys Hammond, David G Jones, Eugene T Grygielko, Jeffrey D Bray, Scott K Thompson
Affiliations

2-Amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2',3':4,5]thieno[2,3-b]pyridine derivatives as selective progesterone receptor agonists

Yonghui Wang et al. Bioorg Med Chem Lett. .

Abstract

High throughput screening of the corporate compound collection led to the identification of a novel series of 2-amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2',3':4,5]thieno[2,3-b]pyridine derivatives as selective PR agonists. Initial SAR exploration leading to potent and selective agonists 9 and 11, X-ray crystal structure of 9 bound to PR-LBD and preliminary developability data are described.

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