Anti-AIDS agents - XXVII. Synthesis and anti-HIV activity of betulinic acid and dihydrobetulinic acid derivatives
Anti-AIDS agents - XXVII. Synthesis and anti-HIV activity of betulinic acid and dihydrobetulinic acid derivatives
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DOI：
10.1016/s0968-0896(97)00158-2
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发表时间：
1997-12-01
影响因子：
3.5
通讯作者：
Lee, KH
中科院分区：
文献类型：
--
作者：
Hashimoto, F;Kashiwada, Y;Lee, KH
基于白桦脂酸（1）和二氢白桦脂酸（9）被鉴定为抗HIV药物的事实，合成了两个系列的羽扇烷型三萜酸衍生物，并评价了它们在急性感染的H9细胞中对HIV-1复制的抑制活性。在这些衍生物中，3-O-（3 '，3'-二甲基琥珀酰基）-桦木酸（3）和3-O-（3 '，3'-二甲基琥珀酰基）-二氢桦木酸（11）均表现出极强的抑制活性，其EC 50值为
Two series of lupane-type triterpenoic acid derivatives were synthesized and evaluated for their inhibitory activity against HIV-1 replication in acutely infected H9 cells, based on the fact that betulinic acid (1) and dihydrobetulinic acid (9) were identified as anti-HIV agents. Among the derivatives, 3-O-(3',3'-dimethylsuccinyl)-betulinic acid (3) and 3-O-(3',3'-dimethylsuccinyl)-dihydrobetulinic acid (11) both demonstrated extremely potent inhibitory activity with EC50 values of