5-alkyl 1,2-dihydrochromeno[3,4-f]quinolines:: A novel class of nonsteroidal progesterone receptor modulators

被引：20

作者：

Zhi, L

Tegley, CM

Edwards, JP

West, SJ

Marschke, KB

Gottardis, MM

Mais, DE

Jones, TK

机构：

[1] Ligand Pharmaceut Inc, Dept Med Chem, San Diego, CA 92121 USA

[2] Ligand Pharmaceut Inc, New Leads Discovery, San Diego, CA 92121 USA

[3] Ligand Pharmaceut Inc, Endocrine Res, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 23期

关键词：

D O I：

10.1016/S0960-894X(98)00608-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of nonsteroidal human progesterone receptor (hPR) agonists, 5-alkyl 1,2-dihydrochromeno[3,4-f]quinolines, was synthesized and evaluated in cotransfection and competitive receptor binding assays. The 5-alkyl substitution was shown to be responsible for the agonist activity and substitution at C9 dramatically enhanced the potency. A number of analogues in this series showed activities similar to or better than progesterone in the cotransfection and binding assays and analogue 15 exhibited similar in vivo activity as medroxyprogesterone acetate (MPA) in murine uterine wet weight/mammary gland morphology assays. (C) 1998 Elsevier Science Ltd. All rights reserved.

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页码：3365 / 3370

页数：6

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