Kashiwada Y, Chiyo J, Ikeshiro Y, Nagao T, Okabe H, Cosentino L M, Fowke K, Lee K H
Niigata College of Pharmacy, Japan.
Bioorg Med Chem Lett. 2001 Jan 22;11(2):183-5. doi: 10.1016/s0960-894x(00)00635-1.
Four isomers of 3,28-di-O-(dimethylsuccinyl)-betulin were prepared and evaluated for anti-HIV activity against HIV-1 replication in H9 lymphocyte cells. 3-O-(3',3'-Dimethylsuccinyl)-28-O-(2", 2"-dimethvlsuccinyl)-betulin (11) was the most potent anti-HIV compound with an EC5, value of 0.00087 microM and a TI value of 42,400.
制备了3,28-二-O-(二甲基琥珀酰基)-桦木醇的四种异构体，并评估了它们对H9淋巴细胞中HIV-1复制的抗HIV活性。3-O-(3',3'-二甲基琥珀酰基)-28-O-(2",2"-二甲基琥珀酰基)-桦木醇(11)是最有效的抗HIV化合物，其EC50值为0.00087微摩尔，TI值为42400。
