937669-57-3

Upstream product

• 32807-28-6 Methyl 4-chloroacetoacetate 
• 103-71-9 phenyl isocyanate 

Downstream Products

• 1402055-52-0 methyl 5-((1H-pyrrolo[2,3-b]pyridin-3-yl)methylene)-4-oxo-2-(phenylamino)-4,5-dihydrofuran-3-carboxylate 
• 1314653-76-3 methyl 5-amino-7-(p-bromophenyl)-2-{[p-bromophenyl(hydroxy)methyl](phenyl)amino}-4,6-di-cyano-1-benzofuran-3-carboxylate 
• 1314653-75-2 methyl 5-amino-7-(p-chlorophenyl)-2-{[p-chlorophenyl(hydroxy)methyl](phenyl)amino}-4,6-dicyano-1-benzofuran-3-carboxylate 

Relevant academic research and scientific papers

FURANONE DERIVATES AND METHODS OF USE THEREOF

Herein disclosed are compounds, compositions, kits, and methods of treating cancers using 7-azaindolyl furanone/thiophene derivatives. These derivatives inhibit serine-threonine kinase Cdc7, a recognized anticancer target affecting DNA replication. Further, the compounds disclosed herein possess potent inhibitory activity in the presence of adenosine triphosphate (ATP), demonstrate significant kinase selectivity, and offer advantages over known Cdc7 inhibitors with prolonged half-life and inhibitory effects.

Discovery of novel furanone derivatives as potent Cdc7 kinase inhibitors

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.