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Caffeoylglycolic and caffeoylamino acid derivatives, halfmers of l-chicoric acid, as new HIV-1 integrase inhibitors

2007; Elsevier BV; Volume: 42; Issue: 10 Linguagem: Inglês

10.1016/j.ejmech.2007.02.016

1768-3254

Seung Uk Lee, Cha‐Gyun Shin, Chong-Kyo Lee, Yong Sup Lee,

Biochemical and Molecular Research

Human immunodeficiency virus (HIV) integrase (IN) catalyzes the integration of HIV DNA copy into the host cell DNA. l-Chicoric acid (1) has been found to be one of the most potent HIV-1 integrase inhibitor. Caffeoylglycolic and caffeoylamino acid derivatives' halfmeric structures of l-chicoric acid 2 were synthesized for the purpose of simplifying the structure of l-chicoric acid. Among synthesized, compounds 2c and 3f showed HIV-1 IN inhibitory activities with IC50 values of 10.5 and 12.0 μM, respectively, comparable to that of parent compound l-chicoric acid (IC50 = 15.7 μM).