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

被引：321
|
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
收藏
页码：4451 / 4455
页数：5
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