非甾体米非司酮模拟物的发现：基于吡唑啉的孕酮受体拮抗剂。
Discovery of non-steroidal mifepristone mimetics: pyrazoline-based PR antagonists.
作者信息
Jones David G, Liang Xi, Stewart Eugene L, Noe Robert A, Kallander Lara S, Madauss Kevin P, Williams Shawn P, Thompson Scott K, Gray David W, Hoekstra William J
机构信息
GlaxoSmithKline, Research Triangle Park, NC 27709-3398, USA.
出版信息
Bioorg Med Chem Lett. 2005 Jul 1;15(13):3203-6. doi: 10.1016/j.bmcl.2005.05.001.
Mifepristone is a non-selective antagonist of 3-oxosteroid receptors with both abortifacient and anti-endometriotic activities. Non-steroidal mimetics of mifepristone and progesterone are important templates for modulation of the progesterone receptor (PR). For our PR program, we sought an unexplored, synthetically accessible non-steroidal mimetic of mifepristone, suitable for parallel synthesis of analogues. Docking of compounds into a PR homology model identified 4-substituted pyrazolines, which, when synthesized and tested, exhibited functional antagonism of PR.
米非司酮是一种3-氧代甾体受体的非选择性拮抗剂，具有堕胎和抗子宫内膜异位活性。米非司酮和孕酮的非甾体模拟物是调节孕酮受体（PR）的重要模板。对于我们的PR项目，我们寻找一种未被探索的、可通过合成获得的米非司酮非甾体模拟物，适用于类似物的平行合成。将化合物对接至PR同源模型中鉴定出4-取代的吡唑啉，合成并测试时，其表现出PR的功能性拮抗作用。
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