具有强效抗HIV活性的新型桦木酸-核苷杂合物
Novel Betulinic Acid-Nucleoside Hybrids with Potent Anti-HIV Activity.
作者信息
Wang Qiang, Li Yujiang, Zheng Liyun, Huang Xiaowan, Wang Yanli, Chen Chin-Ho, Cheng Yung-Yi, Morris-Natschke Susan L, Lee Kuo-Hsiung
机构信息
High & New Technology Research Center of Henan Academy of Sciences, Zhengzhou 450002, China.
National Health Commission Key Laboratory of Birth Defect Prevention, Zhengzhou 450002, China.
出版信息
ACS Med Chem Lett. 2020 Sep 9;11(11):2290-2293. doi: 10.1021/acsmedchemlett.0c00414. eCollection 2020 Nov 12.
Abstract
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 (IC = 0.0078 μM, CC = 9.6 μM) and (IC = 0.020 μM, CC = 23.8 μM) showed more potent or equipotent, respectively, anti-HIV activity but displayed lower cytotoxicity.
摘要
合成了新型桦木酸/桦木酮酸-核苷杂合物作为可能的新型抗HIV药物。在合成的杂合物中，有两种化合物对HIV具有高效性。与齐多夫定（AZT）和双脱氧双氢胸苷（DSB）相比，化合物（IC = 0.0078 μM，CC = 9.6 μM）和（IC = 0.020 μM，CC = 23.8 μM）分别显示出更强或相当的抗HIV活性，但细胞毒性较低。
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