Irie, Takayuki; Asami, Tokiko; Sawa, Ayako; Uno, Yuko; Hanada, Mitsuharu; Taniyama, Chika; Funakoshi, Yoko; Masai, Hisao; Sawa, Masaaki published the artcile< Discovery of novel furanone derivatives as potent Cdc7 kinase inhibitors>, SDS of cas: 112-63-0, the main research area is anticancer Cdc7 kinase inhibition furanone; mol modeling anticancer Cdc7 kinase inhibition furanone; furanone preparation human anticancer Cdc7 kinase inhibition mol binding; Anticancer activity; Apoptosis; Cell cycle; Furanone; Kinase inhibitors; Slow binding.
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 I 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 I potently inhibited Cdc7 activity in cancer cells, and effectively induced cell death.
European Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, SDS of cas: 112-63-0.
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