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Issue 4, 2015
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Synthesis and biological evaluation of pentanedioic acid derivatives as farnesyltransferase inhibitors

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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.

Graphical abstract: Synthesis and biological evaluation of pentanedioic acid derivatives as farnesyltransferase inhibitors

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Supplementary files

Article information


Submitted
03 Nov 2014
Accepted
02 Jan 2015
First published
05 Jan 2015

Med. Chem. Commun., 2015,6, 671-676
Article type
Concise Article
Author version available

Synthesis and biological evaluation of pentanedioic acid derivatives as farnesyltransferase inhibitors

L. Yang, W. Liu, H. Mei, Y. Zhang, X. Yu, Y. Xu, H. Li, J. Huang and Z. Zhao, Med. Chem. Commun., 2015, 6, 671
DOI: 10.1039/C4MD00498A

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