Abstract
Anti HIV-1 active coumarins with either an alkyl or a phenyl group at the 4 position in the coumarin skeleton were isolated from Calophyllum genus (Guttiferae). This review describes on the chemistry of the anti HIV-1 active Calophyllum coumarins : isolation, structure, relative and absolute stereochemistries, synthesis including asymmetric synthesis, anti HIV-1 activity, and structure-activity relationship. The structural modifications indicated that the stereochemistries of the 2, 3-dimethyl-4-chromanol ring in their molecules should play an important role for the activity. Thus, among Calophyllum coumarins (+) -calanolide A (1) and (+) -inophyllum B (8) with all trans configurations (10R, 11S, 12 S) are the most promising candidates for anti HIV-1 active drugs against AIDS.
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