Thyroid receptor ligands.: Part 5:: Novel bicyclic agonist ligands selective for the thyroid hormone receptor β

被引：21

作者：

Collazo, AMG ^{[1
]}

Koehler, KF ^{[1
]}

Garg, N ^{[1
]}

Färbegårdh, M ^{[1
]}

Husman, B ^{[1
]}

Ye, L ^{[1
]}

Ljunggren, J ^{[1
]}

Mellström, K ^{[1
]}

Sandberg, J ^{[1
]}

Grynfarb, M ^{[1
]}

Ahola, H ^{[1
]}

Malm, J ^{[1
]}

机构：

[1] Karo Bio AB, Novum, SE-14157 Huddinge, Sweden

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 05期

关键词：

thyroid hormone receptor agonist; TR beta-selectivity; indole; indane; quinoline; X-ray;

D O I：

10.1016/j.bmcl.2005.11.077

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Based on the examination of the crystal structure of rat TR beta complexed with 3,5,3'-triiodo-L-thyronine (2) a novel TR beta-selective indole derivative 6b was prepared and tested in vitro. This compound was found to be 14 times selective for TR beta over TR alpha in binding and its beta-selectivity could be rationalized through the comparison of the X-ray crystallographic structures of 6b complexed with TR alpha and TR beta. (C) 2005 Elsevier Ltd. All rights reserved.

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页码：1240 / 1244

页数：5

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