新型非甾体孕酮受体配体的合成与构效关系
Synthesis and structure-activity relationships of new non-steroidal progesterone receptor ligands.
作者信息
Kurihara K, Tanabe K, Yamamoto Y, Shinei R, Ajito K, Okonogi T
机构信息
Drug Discovery, Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., Yokohama, Japan.
出版信息
Bioorg Med Chem Lett. 1999 Jul 5;9(13):1837-42. doi: 10.1016/s0960-894x(99)00275-9.
In order to study structure-activity relationships, a series of new non-steroidal progesterone receptor ligands based on PF1092A was synthesized with structural modifications (mostly introduction or removal of a methyl group) at the 3-, 4-, 5-, 7- or 9-position in the 6-acetoxy-4a, 5, 6, 7-tetrahydro-3, 4a, 5-trimethylnaphtho[2,3-b]furan-2(4H)-one skeleton. Critical positions for high binding affinity to the progesterone receptor were identified.
为了研究构效关系，基于PF1092A合成了一系列新的非甾体孕酮受体配体，在6-乙酰氧基-4a,5,6,7-四氢-3,4a,5-三甲基萘并[2,3-b]呋喃-2(4H)-酮骨架的3-、4-、5-、7-或9-位进行了结构修饰（主要是引入或去除一个甲基）。确定了对孕酮受体具有高结合亲和力的关键位置。
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