Synthesis and anti-HIV activity of dibenzylbutyrolactone lignans

LM Yang, SJ Lin, TH Yang, KH Lee

Index: Yang, Li-Ming; Lin, Shwu-Jiuan; Yang, Tsang-Hsiung; Lee, Kuo-Hsiung Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 8 p. 941 - 944

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Citation Number: 45

Abstract

Five optically active dibenzylbutyrolactone lignans were synthesized through a lipase- catalyzed transesterification route, and evaluated for their inhibitory activity against HIV-1 replication in acutely infected H9 cells. Compounds 1 and 2 demonstrated anti-HIV replication activity with an EC50 values of 2.2 and 0.16 μg/ml and a therapeutic index values of 9.1 and 5, respectively. Structure-antiviral activity relationships are discussed.

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