221121-35-3

Upstream product

• 64-17-5 ethanol 
• 1621689-64-2 5-(2-(2-fluorophenyl)-1-hydroxyethylidene)-2,2-dimethyl-1,3-dioxane-4,6-dione 
• 451-81-0 2-(2-fluorophenyl)acetyl chloride 
• 6148-64-7 ethyl potassium malonate 
• 221121-28-4 2-(2-Fluoro-phenyl)-1-imidazol-1-yl-ethanone 

Downstream Products

• 1449299-91-5 N-{4-[2-amino-5-(3,4-dimethoxyphenyl)pyridin-3-yl]phenyl}-5-(2-fluorophenyl)-4-oxo-1-(2,2,2-trifluoroethyl)-1,4-dihydropyridine-3-carboxamide 
• 1449301-03-4 5-(2-fluorophenyl)-4-oxo-1-(2,2,2-trifluoroethyl)-1,4-dihydropyridine-3-carboxylic acid 
• 1449301-01-2 ethyl 5-(2-fluorophenyl)-4-oxo-1-(2,2,2-trifluoroethyl)-1,4-dihydropyridine-3-carboxylate 
• 1449301-78-3 ethyl 5-(2-fluorophenyl)-4-oxo-1,4-dihydropyridine-3-carboxylate 
• 221121-52-4 6-(2-fluoro-benzyl)-2-thioxo-2,3-dihydro-1H-pyrimidin-4-one 

Relevant academic research and scientific papers

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.

5-alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3,4-dihydropyrimidin- 4(3H)-ones: Novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives

Molecular modeling analysis of compounds belonging to the recently published series of dihydro-alkoxy-benzyl-oxopyrimidines (DABOs), such as S- DABOs and DATNOs, gave support to the design of new 2,6-disubstituted benzyl- DABO derivatives as highly potent