Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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First Discovery of Tylophora Alkaloids as HIV Inhibitors

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

Graphical Abstract:


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.

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

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Article Details

VOLUME: 12
ISSUE: 4
Year: 2015
Page: [277 - 283]
Pages: 7
DOI: 10.2174/1570180811666141009235124
Price: $58