Synthesis and biological evaluation of pentanedioic acid derivatives as farnesyltransferase inhibitors

Liuqing Yang; Wei Liu; Hanbing Mei; Yuan Zhang; Xiaojuan Yu; Yufang Xu; Honglin Li; Jin Huang; Zhenjiang Zhao

doi:10.1039/c4md00498a

Synthesis and biological evaluation of pentanedioic acid derivatives as farnesyltransferase inhibitors

Liuqing Yang
, Wei Liu
, Hanbing Mei
, Yuan Zhang
, Xiaojuan Yu
, Yufang Xu
, Honglin Li^*
, Jin Huang
, Zhenjiang Zhao

^*Corresponding author for this work

East China University of Science and Technology

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

14 Scopus citations

Abstract

Structure-based virtual screening of a commercial library identified pentanedioic acid derivatives (6 and 13b) as a kind of novel scaffold farnesyltransferase inhibitors (FTIs). Chemical modifications of the lead compounds, biological assays and analysis of the structure-activity relationships (SAR) were conducted to discover more potent FTIs. Some of them displayed excellent inhibition against FTase, and among them, the most active compound 13n with an IC₅₀ value of 0.0029 μM and SAR analysis might be helpful to the discovery of more potent FTIs.

Original language	English
Pages (from-to)	671-676
Number of pages	6
Journal	MedChemComm
Volume	6
Issue number	4
DOIs	https://doi.org/10.1039/c4md00498a
State	Published - 1 Apr 2015
Externally published	Yes

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title = "Synthesis and biological evaluation of pentanedioic acid derivatives as farnesyltransferase inhibitors",

abstract = "Structure-based virtual screening of a commercial library identified pentanedioic acid derivatives (6 and 13b) as a kind of novel scaffold farnesyltransferase inhibitors (FTIs). Chemical modifications of the lead compounds, biological assays and analysis of the structure-activity relationships (SAR) were conducted to discover more potent FTIs. Some of them displayed excellent inhibition against FTase, and among them, the most active compound 13n with an IC50 value of 0.0029 μM and SAR analysis might be helpful to the discovery of more potent FTIs.",

author = "Liuqing Yang and Wei Liu and Hanbing Mei and Yuan Zhang and Xiaojuan Yu and Yufang Xu and Honglin Li and Jin Huang and Zhenjiang Zhao",

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T1 - Synthesis and biological evaluation of pentanedioic acid derivatives as farnesyltransferase inhibitors

AU - Yang, Liuqing

AU - Liu, Wei

AU - Mei, Hanbing

AU - Zhang, Yuan

AU - Yu, Xiaojuan

AU - Xu, Yufang

AU - Li, Honglin

AU - Huang, Jin

AU - Zhao, Zhenjiang

PY - 2015/4/1

Y1 - 2015/4/1

N2 - Structure-based virtual screening of a commercial library identified pentanedioic acid derivatives (6 and 13b) as a kind of novel scaffold farnesyltransferase inhibitors (FTIs). Chemical modifications of the lead compounds, biological assays and analysis of the structure-activity relationships (SAR) were conducted to discover more potent FTIs. Some of them displayed excellent inhibition against FTase, and among them, the most active compound 13n with an IC50 value of 0.0029 μM and SAR analysis might be helpful to the discovery of more potent FTIs.

AB - Structure-based virtual screening of a commercial library identified pentanedioic acid derivatives (6 and 13b) as a kind of novel scaffold farnesyltransferase inhibitors (FTIs). Chemical modifications of the lead compounds, biological assays and analysis of the structure-activity relationships (SAR) were conducted to discover more potent FTIs. Some of them displayed excellent inhibition against FTase, and among them, the most active compound 13n with an IC50 value of 0.0029 μM and SAR analysis might be helpful to the discovery of more potent FTIs.

UR - https://www.scopus.com/pages/publications/84928033795

U2 - 10.1039/c4md00498a

DO - 10.1039/c4md00498a

M3 - 文章

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SN - 2040-2503

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SP - 671

EP - 676

JO - MedChemComm

JF - MedChemComm

IS - 4

ER -

Synthesis and biological evaluation of pentanedioic acid derivatives as farnesyltransferase inhibitors

Abstract

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