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^*

^*Corresponding author for this work

Peking University
United States Food and Drug Administration

Research output: Contribution to journal › Article › peer-review

80 Scopus citations

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.

Original language	English
Pages (from-to)	2162-2167
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	8
DOIs	https://doi.org/10.1016/j.bmcl.2009.02.116
State	Published - 15 Apr 2009
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Acylhydrazones
Antiviral activity
HIV-1 capsid
Synthesis

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10.1016/j.bmcl.2009.02.116

Cite this

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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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day = "15",

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

language = "英语",

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pages = "2162--2167",

journal = "Bioorganic and Medicinal Chemistry Letters",

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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

Abstract

UN SDGs

Keywords

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