Structure-activity study of retinoid agonists bearing substituted dicarba-closo-dodecaborane.: Relation between retinoidal activity and conformation of two aromatic nuclei

被引：37

作者：

Endo, Y

Iijima, T

Yaguchi, K

Kawachi, E

Inoue, N

Kagechika, H

Kubo, A

Itai, A

机构：

[1] Univ Tokyo, Grad Sch Pharmaceut Sci, Bunkyo Ku, Tokyo 1130033, Japan

[2] Key Mol Inc, Inst Med Mol Design, Bunkyo Ku, Tokyo 1130033, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(01)00204-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have investigated the structure-activity relationships of the potent retinoid agonist, 4-[4-(2-propyl-1,2-dicarba-closo-dodecaboran-1-yl)phenylamino]benzoic acid (BR403), which we have previously reported. Substitution of a methyl group on the aromatic nucleus or a methyl group on the nitrogen atom, or replacement of the amino group with ether, methylene, carboxyl or 1,1-ethylene greatly decreased the activity. The relatively planar conformation at the phenyl-N-phenyl moiety seems to play a critical role in the appearance of the biological activity. (C) 2001 Elsevier Science Ltd. All rights reserved.

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页码：1307 / 1311

页数：5

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