First Discovery of Tylophora Alkaloids as HIV Inhibitors

Title:First Discovery of Tylophora Alkaloids as HIV Inhibitors

Volume: 12 Issue: 4

Author(s): Ziwen Wang, Mingxiao Wang, Lei Wang, Xue Yao, Yue Li, Juan Tan, Wentao Qiao, Yunqi Geng, Yuxiu Liu and Qingmin Wang

Affiliation:

Keywords: AIDS, anti-HIV activity, HIV inhibitor, natural product, structure-activity relationship, tylophora alkaloids.

Abstract: A series of tylophora alkaloids and their derivatives (1–38) were synthesized and systematically bioassayed for their anti-HIV activity for the first time. The results revealed that most of these alkaloids possess good HIV inhibitory effect. Especially, compounds 1, 4 and 25 displayed low nanomolar levels of anti-HIV activity (inhibitory effect at 50 nM: 1: 71%; 4: 60%; 25: 64%), which is about similar to that of the first HIV inhibitor AZT (inhibitory effect at 50 nM: 70%) and slightly lower than that of the first HIV integrase inhibitor MK-0518 (inhibitory effect at 50 nM: 82%). Present studies provide fundamental support for the development of tylophora alkaloids as novel HIV inhibitors.

Cite this article as:

Wang Ziwen, Wang Mingxiao, Wang Lei, Yao Xue, Li Yue, Tan Juan, Qiao Wentao, Geng Yunqi, Liu Yuxiu and Wang Qingmin, First Discovery of Tylophora Alkaloids as HIV Inhibitors, Letters in Drug Design & Discovery 2015; 12 (4) . https://dx.doi.org/10.2174/1570180811666141009235124