MedChemComm p. 671 - 676 (2015)
Update date:2022-07-29
Topics: -Synthesis -Derivatives -Biological evaluation -Inhibitors
Yang, Liuqing
Liu, Wei
Mei, Hanbing
Zhang, Yuan
Yu, Xiaojuan
Xu, Yufang
Li, Honglin
Huang, Jin
Zhao, Zhenjiang
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. This journal is
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