Synthesis and biological activity of 2-methyl-20-EPI analogues of 1α,25-dihydroxyvitamin D3

被引：36

作者：

Fujishima, T

Liu, ZP

Miura, D

Chokki, M

Ishizuka, S

Konno, K

Takayama, H ^{[1
]}

机构：

[1] Teikyo Univ, Fac Pharmaceut Sci, Sagamiko, Kanagawa 1990195, Japan

[2] Teijin Ltd, Inst Biomed Res, Hino, Tokyo 1910065, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(98)00363-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Synthesis and biological evaluation of all eight possible A-ring diastereomers of 2-methyl-20-epi-1,25-dihydroxyvitamin D-3 are described. Among the analogues synthesized, 2 alpha-methyl-20-epi-1 alpha,25-dihydroxyvitamin D-3 exhibited exceptionally high potency. The double modification of 2-methyl substitution and 20-epimerization yielded analogues with unique activity profiles. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：2145 / 2148

页数：4

共 15 条

[1] 20-EPI-VITAMIN-D3 ANALOGS - A NOVEL CLASS OF POTENT REGULATORS OF CELL-GROWTH AND IMMUNE-RESPONSES [J].