Synthesis and HIV-1 integrase inhibition of novel bis-or tetra-coumarin analogues

CC Chiang, JF Mouscadet, HJ Tsai, CT Liu…

Index: Chiang, Chih-Chia; Mouscadet, Jean-Francois; Tsai, Hou-Jen; Liu, Chi-Tsan; Hsu, Ling-Yih Chemical and Pharmaceutical Bulletin, 2007 , vol. 55, # 12 p. 1740 - 1743

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Citation Number: 24

Abstract

Present studies were undertaken on the preparation of synthetic analogues of bis-or tetra- coumarins and their activity against HIV-1 integrase (HIV-1 IN). Among these coumarin analogues, compounds 14, 16 and 18 were found to be potent molecules against HIV-1 IN at IC 50 values of 0.96, 0.58, and 0.49 μM, respectively. The results provided a tool for guiding the further design of more potent antiviral agents and for predicting the affinity of ...