Design and synthesis of novel nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors from caffeic acid phenethyl ester

…, T Sanches, Y Zhong, B Liu, J Xiong, N Neamati…

Index: Wang, Peng; Liu, Chuan; Sanches, Tino; Zhong, Yuan; Liu, Bo; Xiong, Junlong; Neamati, Nouri; Zhao, Guisen Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 16 p. 4574 - 4578

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Citation Number: 14

Abstract

A series of nitrogen-containing polyhydroxylated aromatics from caffeic acid phenethyl ester were designed and synthesized as HIV-1 integrase inhibitors. Most of these compounds exhibited potent inhibitory activities at micromolar concentrations against HIV-1 integrase in the 3′-end processing and the strand transfer. Their key structure–activity relationship was also discussed.

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