期刊
MEDCHEMCOMM
卷 6, 期 4, 页码 671-676出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c4md00498a
关键词
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资金
- Fundamental Research Funds for the Central Universities
- National Natural Science Foundation of China [81102375, 21372078, 81302697, 81222046, 81230076]
- Shanghai Committee of Science and Technology [14431902400]
- 863 Hi-Tech Program of China [2012AA020308]
- Shanghai Rising-Star Tracking Program [13QH1401100]
- Innovation Program of Shanghai Municipal Education Commission [13SG32]
- Fok Ying Tung Education Foundation [141035]
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 mu M and SAR analysis might be helpful to the discovery of more potent FTIs.
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