1620085-54-2

Upstream product

• 5324-30-1 diethyl 2-bromoethylphosphonate 
• 1620085-51-9 4-(2-(4-ethynylphenyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl)pyridin-2(1H)-one 
• 196302-98-4 2-azidoethylphosphonic acid diethyl ester 
• 63697-96-1 4-Ethynylbenzaldehyde 
• 1620085-50-8 1-(4-fluorophenyl)-2-(2-oxo-1,2-dihydropyridin-4-yl)ethane-1,2-dione 

Relevant academic research and scientific papers

Synthesis and structure-activity relationships of 4-fluorophenyl-imidazole p38α MAPK, CK1δ and JAK2 kinase inhibitors

The synthesis and structure-activity relationships of novel 4-(4′-fluorophenyl)imidazoles as selective p38α MAPK, CK1δ and JAK2 inhibitors with improved water solubility are described. Microwave-assisted multicomponent reactions afforded 4-fluorophenyl-2,5- disubstituted imidazoles. Carboxylate and phosphonate groups were introduced via 'click' reactions. The kinase selectivity was influenced by the heteroaryl group at imidazole C-5 and the position of a carboxylic acid or tetrazole at imidazole C-2. For example, pyrimidines 15 and 34 inhibited p38α MAPK with IC50 = 250 nM and 96 nM, respectively. Pyridine 3 gave CK1δ inhibition with IC50 = 89 nM and pyridin-2-one 31 gave JAK2 inhibition with IC50 = 62 nM.