Synthesis and evaluation of anti-HIV activity of isatin beta-thiosemicarbazone derivatives |
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| Authors: | Bal Tanushree Ratan Anand Balasubramani Yogeeswari Perumal Sriram Dharmarajan |
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| Institution: | Medicinal Chemistry Research Laboratory, Pharmacy group, Birla Institute of Technology and Science, Pilani 333031, India. |
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| Abstract: | On the basis of pharmacophoric modelling studies of existing NNRTIs, a series of isatin beta-thiosemicarbazone derivatives was synthesized and evaluated for their anti-HIV activity in HTLV-III(B) 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 EC(50) value of 2.62 microM and a selectivity index of 17.41, while not being cytotoxic to the cell line at a CC(50) value of 44.90 microM. Other tested compounds exhibited marked activity below their toxicity threshold. |
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