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Synthesis and biological evaluation of andrographolide derivatives as potent anti-HIV agents
Authors:Tang Chunlei  Liu Yajuan  Wang Bin  Gu Guolong  Yang Liumeng  Zheng Yongtang  Qian Hai  Huang Wenlong
Affiliation:Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, P. R. China.
Abstract:
In an attempt to develop potent anti-HIV drugs, 20 andrographolide derivatives were designed, synthesized, and evaluated for their in vitro anti-HIV activity. The screening results revealed that five compounds showed potent anti-HIV activities with therapeutic indices (TI) above 10. The most promising compound 6f shows a significant TI close to 34.07, with the potency to be a new lead.
Keywords:Andrographolide derivatives  Anti‐HIV  Synthesis
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