European Journal of Medicinal Chemistry p. 406 - 418 (2017)
Update date:2022-09-26
Topics:
Irie, Takayuki
Asami, Tokiko
Sawa, Ayako
Uno, Yuko
Hanada, Mitsuharu
Taniyama, Chika
Funakoshi, Yoko
Masai, Hisao
Sawa, Masaaki
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.
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