Novel Betulinic Acid-Nucleoside Hybrids with Potent Anti-HIV Activity. 2020

Qiang Wang, and Yujiang Li, and Liyun Zheng, and Xiaowan Huang, and Yanli Wang, and Chin-Ho Chen, and Yung-Yi Cheng, and Susan L Morris-Natschke, and Kuo-Hsiung Lee
High & New Technology Research Center of Henan Academy of Sciences, Zhengzhou 450002, China.

Novel betulinic/betulonic acid-nucleoside hybrids were synthesized as possible new anti-HIV agents. Among the synthesized hybrids, two compounds were highly effective against HIV. Compared with AZT and DSB, compounds 10a (IC50 = 0.0078 μM, CC50 = 9.6 μM) and 10b (IC50 = 0.020 μM, CC50 = 23.8 μM) showed more potent or equipotent, respectively, anti-HIV activity but displayed lower cytotoxicity.

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