Synthesis and structure-activity relationships of new non-steroidal progesterone receptor ligands

被引:20
作者
Kurihara, K [1 ]
Tanabe, K [1 ]
Yamamoto, Y [1 ]
Shinei, R [1 ]
Ajito, K [1 ]
Okonogi, T [1 ]
机构
[1] Meiji Seika Kaisha Ltd, Pharmaceut Res Ctr, Drug Discovery, Kohoku Ku, Yokohama, Kanagawa 2228567, Japan
关键词
D O I
10.1016/S0960-894X(99)00275-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In order to study structure-activity relationships, a series of new non-steroidal progesterone receptor ligands based on PF1092A (1)) 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 (2)) skeleton. Critical positions for high binding affinity to the progesterone receptor were identified. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1837 / 1842
页数:6
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