疣孢菌素D衍生物的合成及其抗微管蛋白活性

Synthesis and anti-tubulin activity of ustiloxin D derivatives.

作者信息

Morisaki N, Mitsui Y, Yamashita Y, Koiso Y, Shirai R, Hashimoto Y, Iwasaki S

机构信息

Institute of Molecular and Cellular Biosciences, University of Tokyo, Japan.

出版信息

J Antibiot (Tokyo). 1998 Apr;51(4):423-7. doi: 10.7164/antibiotics.51.423.

DOI:10.7164/antibiotics.51.423

PMID:9630864

Abstract

Ustiloxin D, produced by the rice plant pathogen Ustilaginoidea virens, exhibits potent anti-tubulin activity. In order to elucidate the effects of functional groups in ustiloxin D on its activity, several derivatives were synthesized and their anti-tubulin activities were estimated. The N,N-dimethylamino derivative and the 14-O-methyl derivative were inactive (IC50 > 50 microM). 20-Hydroxymethylated ustiloxin D showed decreased inhibitory activity compared with ustiloxin D.

摘要

稻瘟病菌产生的稻曲毒素D具有强大的抗微管蛋白活性。为了阐明稻曲毒素D中官能团对其活性的影响，合成了几种衍生物并评估了它们的抗微管蛋白活性。N，N-二甲基氨基衍生物和14-O-甲基衍生物无活性（IC50>50 microM）。与稻曲毒素D相比，20-羟甲基化的稻曲毒素D显示出降低的抑制活性。