Synthesis and evaluation of anti-HIV activity of isatin β-thiosemicarbazone derivatives

被引：309

作者：

Bal, TR ^{[1
]}

Anand, B ^{[1
]}

Yogeeswari, P ^{[1
]}

Sriram, D ^{[1
]}

机构：

[1] Birla Inst Technol & Sci, Med Chem Res Lab, Pharm Grp, Pilani 333031, Rajasthan, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 20期

关键词：

anti-HIV; isatin; thiosemicarbazones;

D O I：

10.1016/j.bmcl.2005.07.046

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

On the basis of pharmacophoric modelling studies of existing NNRTIs, a series of isatin beta-thiosemicarbazonc derivatives was synthesized and evaluated for their anti-HIV activity in HTLV-IIIB strain in the CEM cell line. Three compounds showed significant anti-HIV activity, whereupon compound 6 was found to be the most active compound with an EC50 value of 2.62 mu M and a selectivity index of 17.41, while not being cytotoxic to the cell line at a CC50 value of 44.90 mu M. Other tested compounds exhibited marked activity below their toxicity threshold. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：4451 / 4455

页数：5

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