2-氨基-9-芳基-3-氰基-4-甲基-7-氧代-6,7,8,9-四氢吡啶并[2',3':4,5]噻吩并[2,3-b]吡啶衍生物作为选择性孕酮受体激动剂。
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.
作者信息
Wang Yonghui, Duraiswami Chaya, Madauss Kevin P, Tran Thuy B, Williams Shawn P, Deng Su-Jun, Graybill Todd L, Hammond Marlys, Jones David G, Grygielko Eugene T, Bray Jeffrey D, Thompson Scott K
机构信息
Research & Development, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA.
出版信息
Bioorg Med Chem Lett. 2009 Sep 1;19(17):4916-9. doi: 10.1016/j.bmcl.2009.07.100. Epub 2009 Jul 23.
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.
对公司化合物库进行高通量筛选，鉴定出一系列新型的2-氨基-9-芳基-3-氰基-4-甲基-7-氧代-6,7,8,9-四氢吡啶并[2',3':4,5]噻吩并[2,3-b]吡啶衍生物作为选择性孕激素受体（PR）激动剂。描述了导致强效和选择性激动剂9和11的初步构效关系（SAR）探索、与PR配体结合域（PR-LBD）结合的9的X射线晶体结构以及初步的成药性数据。
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