58337-17-0Relevant 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.
Drug-induced modifications of the immune response. 12. 4,5-Dihydro-4-oxo-2-(substituted amino)-3-furancarboxylic acids and derivatives as novel antiallergic agents
Mck,Zazulak,Radov,baer,Steward,Elzer,Kinsolving,Georgiev
, p. 1910 - 1918 (2007/10/02)
The synthesis of a series of novel 4,5-dihydro-4-oxo-2-(substituted amino)-3-furancarboxylic acids, salts, esters, and amides is described. The title compounds when tested in the mediator-induced dermal vascular permeability and active anaphylaxis assays in rats demonstrated moderate to potent antiallergic activity. The [2-trans-(4-methyl-phenyl)cyclopropyl]amino analogue 53 emerged as the most active derivative. Thus, when administered intraperitoneally to rate at a dose of 100 mg/kg, it inhibited the action of the mediators serotonin, histamine, and bradykinin by 100%. In the active anaphylaxis assay in rats, compound 30 suppressed the edema by 81% at a dose of 100 mg/kg, following intraperitoneal administration.
