Anti-AIDS agents 49. Synthesis, anti-HIV, and anti-fusion activities of IC9564 analogues based on betulinic acid
Anti-AIDS agents 49. Synthesis, anti-HIV, and anti-fusion activities of IC9564 analogues based on betulinic acid
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DOI：
10.1021/jm020069c
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发表时间：
2002-09-12
影响因子：
7.3
通讯作者：
Lee, KH
中科院分区：
文献类型：
--
作者：
Sun, IC;Chen, CH;Lee, KH
白桦酸衍生物IC9564可抑制人类免疫缺陷病毒(HIV)-1入侵。在一系列IC9564衍生物中，5和20是最有希望的抗HIV感染的化合物，其EC50值分别为0.33和0.46um。两种化合物均能抑制合胞体的形成。形成，EC50值分别为0.40和0.33微米。两种检测方法的EC50值具有可比性，表明这些化合物是融合抑制物。构效关系数据还表明，在保持抗HIV活性的同时，可以消除IC9564中的双键，并用L亮氨酸取代他汀类部分。
The betulinic acid derivative IC9564 inhibits human immunodeficiency virus (HIV)-1 entry. Among a series of IC9564 derivatives, 5 and 20 were the most promising compounds against HIV infection with EC50 values of 0.33 and 0.46 muM, respectively. Both compounds inhibited syncytium. formation with EC50 values of 0.40 and 0.33 muM, respectively. The comparable EC50 values in the two assays suggested that these compounds are fusion inhibitors. The structure-activity relationship data also indicated that a double bond in IC9564 can be eliminated and the statine moiety can be replaced with L-leucine while retaining anti-HIV activity.