3148-33-2Relevant academic research and scientific papers
Discovery of novel furanone derivatives as potent Cdc7 kinase inhibitors
Irie, Takayuki,Asami, Tokiko,Sawa, Ayako,Uno, Yuko,Hanada, Mitsuharu,Taniyama, Chika,Funakoshi, Yoko,Masai, Hisao,Sawa, Masaaki
, p. 406 - 418 (2017/03/11)
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 structure-activity 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.
NOVEL FURANONE DERIVATIVE
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Paragraph 0068; 0069; 0070, (2014/02/16)
To provide a novel furanone derivative, and a medicine including the same. The furanone derivative is represented by the formula (I): wherein A represents —COOR1 or a hydrogen atom; R1 represents a hydrogen atom, an optionally substituted hydrocarbon grou
