Chemistry of anti HIV-1 active Calophyllum coumarins

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 thier 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.