Synthesis and biological evaluation of andrographolide derivatives as potent anti-HIV agents |
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Authors: | Tang Chunlei Liu Yajuan Wang Bin Gu Guolong Yang Liumeng Zheng Yongtang Qian Hai Huang Wenlong |
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Affiliation: | Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, P. R. China. |
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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. |
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Keywords: | Andrographolide derivatives Anti‐HIV Synthesis |
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