Bioorganic & medicinal chemistry letters

Synthesis of trans-caffeate analogues and their bioactivities against HIV-1 integrase and cancer cell lines

C Xia, H Li, W Hu

文献索引：Xia, Chun-nian; Li, Hai-bo; liu, Feng; Hu, Wei-xiao Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 24 p. 6553 - 6557

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被引用次数: 31

摘要

Forty caffeate analogues were synthesized via a convenient method starting from vanillin with moderate to good yields. The testing of biological activity of these compounds against HIV-1 integrase indicates that four compounds: bornyl caffeate, bornyl 2-nitrocaffeate, 5- nitrocaffeic acid and 5-nitrocaffeic acid phenethyl ester (5-nitroCAPE) possess a good HIV integrase inhibitory activity, IC50 19.9, 26.8, 25.0 and 13.5 μM, respectively. Twelve ...