Kashiwada Yoshiki, Sekiya Michiko, Ikeshiro Yasumasa, Fujioka Toshihiro, Kilgore Nicole R, Wild Carl T, Allaway Graham P, Lee Kuo-Hsiung
Faculty of Pharmaceutical Sciences, Niigata University of Pharmacy and Applied Life Sciences, Niigata 950-2081, Japan.
Bioorg Med Chem Lett. 2004 Dec 6;14(23):5851-3. doi: 10.1016/j.bmcl.2004.09.033.
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 x 10(-5) microM and a TI value of 1.12 x 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 microM, respectively, and TI values of 16,160 and 19,530, respectively.
制备了3 - O - 酰基 - 桦木醇和 - 二氢桦木醇衍生物，并对其抗HIV活性进行了评估。3 - O - 戊二酰基 - 二氢桦木醇（17）表现出极强的抗HIV活性，其半数有效浓度（EC50）值为2×10^(-5) μM，治疗指数（TI）值为1.12×10^6。3 - O -（3'，3'-二甲基琥珀酰基） - 和3 - O -（3'，3'-二甲基戊二酰基） - 二氢桦木醇（15, 16）也是有效的抗HIV化合物，其EC50值分别为0.0017和0.0013 μM，TI值分别为16,160和19,530。
