904053-21-0Relevant articles and documents
A microwave approach to the synthesis of certain 4-(substituted phenyl)-6-phenyl-3-cyano-2-pyridones
Marinkovic, Aleksandar,Mijin, Du?an,Mirkovic, Jelena,Maslak, Veselin,Kappe, C. Oliver
, p. 759 - 765 (2014)
A study of the synthesis of 4-(substituted phenyl)-6-phenyl-3-cyano- 2-pyridones from ethyl 2-cyano-3-(substituted phenyl) acrylates and acetophenone is presented. The 2-pyridones were obtained using conventional as well as microwave synthesis under solvent and solvent-free conditions in domestic and laboratory microwave ovens. The structure of the obtained pyridones was confirmed by m.p., FT-IR, NMR and UV data.
Discovery of colon tumor cell growth inhibitory agents through a combinatorial approach
Abadi, Ashraf H.,Abouel-Ella, Dalal A.,Lehmann, Jochen,Tinsley, Heather N.,Gary, Bernard D.,Piazza, Gary A.,Abdel-Fattah, Mohammed A.O.
experimental part, p. 90 - 97 (2010/03/24)
Two series with the general formula of 4,6-diaryl-2-oxo-1,2 dihydropyridine-3-carbonitriles and their isosteric 4,6-diaryl-2-imino-1,2-dihydropyridine-3-carbonitrile were synthesized through one pot reaction of the appropriate acetophenone, aldehyde, ammonium acetate with ethyl cyanoacetate or malononitrile, respectively. The synthesized compounds were evaluated for their tumor cell growth inhibitory activity against the human HT-29 colon tumor cell line, as well as their PDE3 inhibitory activity. Compound 4-(2-Ethoxyphenyl)-2-oxo-6-thiophen-3-yl-1,2-dihydropyridine-3 carbonitrile (21) showed tumor cell growth inhibitory activity with an IC50 value of 1.25 μM. Meanwhile, 4-(4-Ethoxyphenyl)-2-imino-6-(thiophen-3-yl)-1,2-dihydropyridine-3-carbonitrile (26) showed inhibitory effect upon PDE3 using cAMP or cGMP as substrate. No correlation exists between PDE3 inhibition and the tumor cell growth inhibitory activity. Docking compound 21 to other possible molecular targets showed the potential to bind PIM1 Kinase.