72676-86-9

Upstream product

• 290-87-9 1,3,5-Triazine 
• 718-08-1 ethyl 3-oxo-4-phenylbutyrate 
• 4693-91-8 4-methoxyphenyl-acetic chloride 
• 4637-24-5 N,N-dimethyl-formamide dimethyl acetal 
• 153525-08-7 5-[1-Hydroxy-2-(4-methoxy-phenyl)-ethylidene]-2,2-dimethyl-[1,3]dioxane-4,6-dione 
• 74965-87-0 2,2-dimethyl-5-(2-phenylacetyl)-1,3-dioxane-4,6-dione 
• 103-80-0 phenylacetyl chloride 

Downstream Products

• 72676-91-6 1-ethyl-5-phenyl-4-oxo-1,4-dihydro-3-pyridinecarboxylic acid 
• 74632-05-6 ethyl 1-phenyl-4-oxo-1,4-dihydro-3-pyridinecarboxylate 
• 1449300-99-5 ethyl 4-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)-1,4-dihydropyridine-3-carboxylate 
• 1449300-97-3 ethyl 1-(2-fluoroethyl)-4-oxo-5-phenyl-1,4-dihydropyridine-3-carboxylate 
• 1355011-60-7 4-oxo-5-phenyl-1,4-dihydropyridine-3-carboxylic acid 
• 1449300-23-5 N-[4-(2-amino-5-{4-[(2R)-1,4-dioxan-2-ylmethoxy]-3-methoxyphenyl}pyridin-3-yl)phenyl]-1-(2-fluoroethyl)-4-oxo-5-phenyl-1,4-dihydropyridine-3-carboxamide 
• 1449300-18-8 N-(4-{2-amino-5-[3-methoxy-4-(2-pyrrolidin-1-ylethoxy)phenyl]pyridin-3-yl}phenyl)-1-(2-fluoroethyl)-4-oxo-5-phenyl-1,4-dihydropyridine-3-carboxamide 
• 1449299-89-1 N-{4-[2-amino-5-(3,4-dimethoxyphenyl)pyridin-3-yl]phenyl}-4-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)-1,4-dihydropyridine-3-carboxamide 
• 1449301-00-1 4-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)-1,4-dihydropyridine-3-carboxylic acid 
• 1449299-88-0 N-{4-[2-amino-5-(3,4-dimethoxyphenyl)pyridin-3-yl]phenyl}-1-(2-fluoroethyl)-4-oxo-5-phenyl-1,4-dihydropyridine-3-carboxamide 
• 1449300-98-4 1-(2-fluoroethyl)-4-oxo-5-phenyl-1,4-dihydropyridine-3-carboxylic acid 
• 244638-39-9 ethyl 4-chloro-3-phenyl-5-pyridinecarboxylate 

Relevant academic research and scientific papers

PYRIDO-AZAHETERECYDIC COMPOUND AND PREPARATION METHOD AND USE THEREOF

The present invention discloses a pyrido-azacyclic compound represented by formula I, an isomer thereof, a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof, a preparation process thereof and a composition comprising the compound, and a use thereof as a multi-target protein kinase inhibitor in the preparation of a medicament for the treatment of diseases that are associated with protein kinase, especially c-Met, such as cancer and the like. The compound represented by formula I has potent inhibitory activity on tumor cells with overexpression of c-Met kinase, can effectively target c-Met-mediated signaling pathway, and can be used in the treatment of diseases such as cancer and the like that is caused by the overexpression of c-Met kinase.

Bioisosteric replacement of an acylureido moiety attached to an indolin-2-one scaffold with a malonamido or a 2/4-pyridinoylamido moiety produces a selectively potent Aurora-B inhibitor

Bioisosteric replacement of acylureido moiety in 6-acylureido-3- pyrrolylmethylidene-2-oxoindoline derivatives resulted in a series of malonamido derivatives with indolin-2-one scaffold (11-14). Further conformational restrictions of the malonamido moiety led to 2-oxo-1,2-dihydropyridine (21-25) or a 4-oxo-1,4-dihydropyridine derivatives (31-36). 4-Oxo-1,4-dihydropyridine derivatives were more potent Aurora B inhibitors than their 2-oxo-1,2- dihydropyridine counterparts and demonstrated cytotoxicities against A549 and HepG2 cells in the submicromolar range. In A549 cells, 31h decreased phosphorylation of histone H3, triggered polyploidy, induced expression of pro-apoptotic Fas and FasL with subsequent activation of caspase 8, resulting into apoptosis. In a Huh7-xenograft mouse model, 31h demonstrated potent in vivo efficacy with a daily dose of 5 mg/kg.