- 3-O-Glutaryl-dihydrobetulin and related monoacyl derivatives as potent anti-HIV agents
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3-O-Glutaryl-dihydrobetulin (17) demonstrated extremely potent anti-HIV activity with an EC50 value of 2 × 10-5 μM and a TI value of 1.12 × 106. 3-O-(3′,3′- Dimethylsuccinyl)- and 3-O-(3′,3′-dimethylglutaryl)-dihydrobetulins (15, 16) were also potent anti-HIV compounds with EC50 values of 0.0017 and 0.0013 μM, respectively, and TI values of 16,160 and 19,530, respectively. 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 EC50 value of 2 × 10-5 μM and a TI value of 1.12 × 106. 3-O-(3′,3′-Dimethylsuccinyl)- and 3-O-(3′,3′- dimethylglutaryl)-dihydrobetulins (15, 16) were also potent anti-HIV compounds with EC50 values of 0.0017 and 0.0013 μM, respectively, and TI values of 16,160 and 19,530, respectively.
- Kashiwada, Yoshiki,Sekiya, Michiko,Ikeshiro, Yasumasa,Fujioka, Toshihiro,Kilgore, Nicole R.,Wild, Carl T.,Allaway, Graham P.,Lee, Kuo-Hsiung
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p. 5851 - 5853
(2007/10/03)
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