Synthesis of 5(6)-dihydro-OSW-1 analogs bearing three kinds of disaccharides linking at 15-hydroxy and their antitumor activities

被引：20

作者：

Guan, Yuyao ^{[1
]}

Zheng, Dan ^{[1
]}

Zhou, Liang ^{[1
]}

Wang, Haixing ^{[1
]}

Yan, Zheng ^{[2
]}

Wang, Nan ^{[2
]}

Chang, Hong ^{[3
]}

She, Pingping ^{[3
]}

Lei, Pingsheng ^{[1
]}

机构：

[1] Chinese Acad Med Sci, Peking Union Med Coll, Inst Mat Med,Minist Educ, Key Lab Bioact Subst & Resources Utilizat Chinese, Beijing 100050, Peoples R China

[2] Chinese Acad Med Sci, Peking Union Med Coll, Inst Mat Med, Dept Pharmacol, Beijing 100050, Peoples R China

[3] Beijing 2nd Senior High Sch, Res Ctr, Beijing 100010, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 10期

基金：

中国国家自然科学基金;

关键词：

5(6)-Dihydro-OSW-1 analogs cholestane; glycosides antitumor activities synthesis; CHOLESTANE GLYCOSIDES; METHYL PROTODIOSCIN; FUROSTAN SAPONIN; INTACT SKELETON; SIDE-CHAINS; OSW-1; CYTOTOXICITY; SAPOGENINS; STEROIDS; STRATEGY;

D O I：

10.1016/j.bmcl.2011.03.065

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

In order to study the SAR of 5(6)-dihydro-OSW-1, eight 15(alpha)beta-O-glycosyl analogs (26-33) carrying three kinds of disaccharides including [beta-D-Xylp-(1-3)-alpha-L-Arap], [beta-D-Xylp-(1-4)-alpha-L-Arap] and [alpha-L-Rhap-(1-2)-(alpha)beta-D-Glcp] were designed and synthesized. Their in vitro antitumor activities were tested by the standard MTT assay which disclosed that compound 33 (IC50 = 0.28-0.52 mu M) showed potential antitumor activities. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：2921 / 2924

页数：4

共 24 条

[1]

Apoptosis induced by dioscin in Hela cells [J].