Synthesis of new chiral 2,5-disubstituted 1,3,4-thiadiazoles possessing γ-butenolide moiety and preliminary evaluation of in vitro anticancer activity

被引：88

作者：

Wei, Meng-Xue ^{[1
,2
]}

Feng, Lei ^{[1
,2
]}

Li, Xue-Qiang ^{[1
,2
]}

Zhou, Xue-Zhang ^{[3
]}

Shao, Zhi-Hui ^{[4
]}

机构：

[1] Ningxia Univ, Key Lab Energy Sources & Chem Engn, Dev Ctr Nat Prod & Medicat, Yinchuan 750021, Peoples R China

[2] Ningxia Univ, Sch Chem & Chem Engn, Yinchuan 750021, Peoples R China

[3] Ningxia Univ, Key Lab Minist Educ Protect & Utilizat Special, Sch Life Sci, Yinchuan 750021, Peoples R China

[4] Yunnan Univ, Key Lab Med Chem Nat Resource, Minist Educ, Kunming 650091, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 44卷 / 08期

基金：

中国国家自然科学基金;

关键词：

1,3,4-Thiadiazoles; Butenolide; X-ray crystallography; Hela cells; Growth inhibitory; ANTIMICROBIAL ACTIVITY; STRUCTURE ELUCIDATION; DYSIDIOLIDE; DERIVATIVES; ANALOGS; ANTICONVULSANT; INHIBITORS; POTENT;

D O I：

10.1016/j.ejmech.2009.03.023

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of chiral 1,3,4-thiadiazoles derivatives possessing gamma-substituted butenolide moiety were synthesized and evaluated for in vitro anticancer properties. All the compounds showed good anticancer activities against Hela cell lines. Of ail the studied compounds, compound Sle exhibited the best inhibitory activity with an IC50 of 0-9 mu M. After being treated with 0.1 mu g/mL compound 9e for 24 h, the growth inhibition rate of Hela cell lines was 59.2%. (C) 2009 Elsevier Masson SAS. All rights reserved.

引用

页码：3340 / 3344

页数：5

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