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

TR Bal, B Anand, P Yogeeswari, D Sriram

Index: Bal, Tanushree Ratan; Anand, Balasubramani; Yogeeswari, Perumal; Sriram, Dharmarajan Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 20 p. 4451 - 4455

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Citation Number: 188

Abstract

On the basis of pharmacophoric modelling studies of existing NNRTIs, a series of isatin β- thiosemicarbazone 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 μM and a selectivity index of 17.41, while not being cytotoxic to the cell line at a ...