期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 130, 期 -, 页码 406-418出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2017.02.030
关键词
Kinase inhibitors; Cell cycle; Apoptosis; Anticancer activity; Furanone; Slow binding
资金
- Grants-in-Aid for Scientific Research [16K14675] Funding Source: KAKEN
Cdc7 is a serine-threonine kinase and plays a conserved and important role in DNA replication, and it has been recognized as a potential anticancer target. Herein, we report the design, synthesis and structureactivity relationship of novel furanone derivatives as Cdc7 kinase inhibitors. Compound 13 was identified as a strong inhibitor of Cdc7 with an IC50 value of 0.6 nM in the presence of 1 mM ATP and showed excellent kinase selectivity. In addition, it exhibited slow off-rate characteristics, which may offer advantages over known Cdc7 inhibitors in its potential to yield prolonged inhibitory effects in vivo. Compound 13 potently inhibited Cdc7 activity in cancer cells, and effectively induced cell death. (C) 2017 Elsevier Masson SAS. All rights reserved.
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