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Synthesis and biological evaluation of andrographolide derivatives as potent anti-HIV agents. 2012
Chunlei Tang, and
Yajuan Liu, and
Bin Wang, and
Guolong Gu, and
Liumeng Yang, and
Yongtang Zheng, and
Hai Qian, and
Wenlong Huang
Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, P. R. China.
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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