3-O-Glutaryl-dihydrobetulin and related monoacyl derivatives as potent anti-HIV agents.

Abstract 3- O -Acyl-betulin and -dihydrobetulin derivatives were prepared and evaluated for anti-HIV activity. 3- O -Glutaryl-dihydrobetulin ( 17 ) demonstrated extremely potent anti-HIV activity with an EC 50 value of 2 × 10 −5  μM and a TI value of 1.12 × 10 6 . 3- O -(3′,3′-Dimethylsuccinyl)- and 3- O -(3′,3′-dimethylglutaryl)-dihydrobetulins ( 15 , 16 ) were also potent anti-HIV compounds with EC 50 values of 0.0017 and 0.0013 μM, respectively, and TI values of 16,160 and 19,530, respectively.