Initial structure-activity relationship of a novel class of nonpeptidyl GnRH receptor antagonists: 2-arylindoles

被引：50
作者：
Chu, L
Hutchins, JE
Weber, AE
Lo, JL
Yang, YT
Cheng, K
Smith, RG
Fisher, MH
Wyvratt, MJ
Goulet, MT
机构：
[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
[2] Merck Res Labs, Dept Biochem & Physiol, Rahway, NJ 07065 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 04期
关键词：
D O I：
10.1016/S0960-894X(00)00707-1
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A nonpeptidyl GnRH receptor antagonist (1), with a unique 2-arylindole core, was identified through the Merck inhouse screening for binding affinity on the rat GnRH receptor. SAR studies directed toward the alkoxy-ethanolamine and 2-aryl groups resulted in a simpler lead structure with improved activity. This compound 50 exhibits a 60-fold improvement in binding activity over our initial lead 1. (C) 2001 Elsevier Science Ltd. All rights reserved.
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页码：509 / 513
页数：5
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