Synthesis and antiviral activities of novel acylhydrazone derivatives targeting HIV-1 capsid protein

Baohe Tian; Meizi He; Shixing Tang; Indira Hewlett; Zhiwu Tan; Jiebo Li; Yinxue Jin; Ming Yang

doi:10.1016/j.bmcl.2009.02.116

Synthesis and antiviral activities of novel acylhydrazone derivatives targeting HIV-1 capsid protein

Baohe Tian
, Meizi He
, Shixing Tang
, Indira Hewlett
, Zhiwu Tan
, Jiebo Li
, Yinxue Jin
, Ming Yang^*

^*此作品的通讯作者

Peking University
United States Food and Drug Administration

科研成果: 期刊稿件 › 文章 › 同行评审

80 引用（Scopus）

摘要

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.

源语言	英语
页（从-至）	2162-2167
页数	6
期刊	Bioorganic and Medicinal Chemistry Letters
卷	19
期	8
DOI	https://doi.org/10.1016/j.bmcl.2009.02.116
出版状态	已出版 - 15 4月 2009
已对外发布	是

联合国可持续发展目标

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title = "Synthesis and antiviral activities of novel acylhydrazone derivatives targeting HIV-1 capsid protein",

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.",

keywords = "Acylhydrazones, Antiviral activity, HIV-1 capsid, Synthesis",

author = "Baohe Tian and Meizi He and Shixing Tang and Indira Hewlett and Zhiwu Tan and Jiebo Li and Yinxue Jin and Ming Yang",

year = "2009",

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doi = "10.1016/j.bmcl.2009.02.116",

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T1 - Synthesis and antiviral activities of novel acylhydrazone derivatives targeting HIV-1 capsid protein

AU - Tian, Baohe

AU - He, Meizi

AU - Tang, Shixing

AU - Hewlett, Indira

AU - Tan, Zhiwu

AU - Li, Jiebo

AU - Jin, Yinxue

AU - Yang, Ming

PY - 2009/4/15

Y1 - 2009/4/15

N2 - 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.

AB - 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.

KW - Acylhydrazones

KW - Antiviral activity

KW - HIV-1 capsid

KW - Synthesis

UR - https://www.scopus.com/pages/publications/63149164406

U2 - 10.1016/j.bmcl.2009.02.116

DO - 10.1016/j.bmcl.2009.02.116

M3 - 文章

C2 - 19297155

AN - SCOPUS:63149164406

SN - 0960-894X

VL - 19

SP - 2162

EP - 2167

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 8

ER -

Synthesis and antiviral activities of novel acylhydrazone derivatives targeting HIV-1 capsid protein

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