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Novel Betulinic Acid–Nucleoside Hybrids with Potent Anti-HIV Activity

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journal contribution
posted on 09.09.2020 by Qiang Wang, Yujiang Li, Liyun Zheng, Xiaowan Huang, Yanli Wang, Chin-Ho Chen, Yung-Yi Cheng, Susan L. Morris-Natschke, Kuo-Hsiung Lee
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.