Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 15, Issue 20, Pages 4451-4455Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.07.046
Keywords
anti-HIV; isatin; thiosemicarbazones
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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.
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