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Absolute configurations of integracins A, B, and 15'-dehydroxy-integracin B
Hai-Li Liu1, Xiao-Yin Huang, Jia Li
1State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, People's Republic of China.
Abstract:
Integracins A (1) and B (2), potent HIV-1 integrase inhibitors, and 15'-dehydroxy-integracin B (3) were isolated for the first time from Chinese mangrove plant Sonneratia hainanensis. Their absolute configurations were determined by the Mosher's method and specific rotation analysis of alcohols (6 and 7) obtained from integracin A in two steps and by chemical correlation. Integracin A (1) also exhibited significant cytotoxicity against the tumor cell lines HepG2 and NCI-H460 with both 100% inhibitions at 25 µg/ml.
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