Synthesis and antiviral activities of novel acylhydrazone derivatives targeting HIV-1 capsid protein |
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| Authors: | Baohe Tian Meizi He Shixing Tang Indira Hewlett Zhiwu Tan Jiebo Li Yinxue Jin Ming Yang |
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| Institution: | 1. State Key Laboratory of Natural and Biomimetic Drugs, Peking University, PO Box 261, Beijing 100191, China;2. Center for Biologics Evaluation and Research, Food and Drug Administration, Bethesda, MD 20892, USA |
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| Abstract: | HIV-1 capsid protein (CA) plays important roles in the viral replication cycle. A number of acylhydrazone derivatives that act as inhibitors of HIV-1 CA assembly, were designed and synthesized. The synthesized compounds were tested for their antiviral activities and cytotoxicities using CEM cells. Some derivatives also were assayed for their ability to inhibit HIV-1 CA assembly in vitro. Among them, compounds 14f and 14i display the most promising potency with EC50 values of 0.21 and 0.17 μΜ, respectively. |
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