基于6-芳基-1,2-二氢-2,2,4-三甲基喹啉构象受限亚系列的非甾体孕酮受体拮抗剂。
Nonsteroidal progesterone receptor antagonists based on a conformationally-restricted subseries of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines.
作者信息
Hamann L G, Winn D T, Pooley C L, Tegley C M, West S J, Farmer L J, Zhi L, Edwards J P, Marschke K B, Mais D E, Goldman M E, Jones T K
机构信息
Department of Medicinal Chemistry, Ligand Pharmaceuticals, San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 1998 Oct 6;8(19):2731-6. doi: 10.1016/s0960-894x(98)00482-x.
A series of nonsteroidal human progesterone receptor (hPR) antagonists based on conformationally-restricted analogues of a 6-aryl-1,2-dihydro-2,2,4-trimethylquinoline pharmacophore were synthesized and evaluated for their ability to bind to the human progesterone receptor and inhibit progesterone-stimulated reporter gene expression in mammalian cells.
基于6-芳基-1,2-二氢-2,2,4-三甲基喹啉药效团的构象受限类似物，合成了一系列非甾体类人孕酮受体（hPR）拮抗剂，并评估了它们与人孕酮受体结合以及抑制哺乳动物细胞中孕酮刺激的报告基因表达的能力。
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