Rational design and synthesis of novel 2-(substituted-2H-chromen-3-yl)-5-aryl-1H-imidazole derivatives as an anti-angiogenesis and anti-cancer agentElectronic supplementary information (ESI) available. See DOI: 10.1039/c4ra09945a

Based on earlier proven pharmacophore analogues of cancer a novel 2-(substituted-2 H -chromen-3-yl)-5-aryl-1 H -imidazoles ( 13-16 ) were rationally designed and synthesized by the reaction of chromene-3-carboxylic acids ( 10a-d ) with substituted acyl bromides in the presence of TEA followed by refluxing with NH 4 OAc in toluene. Compounds 13-16 were screened in vitro for the inhibition of KRAS/Wnt and their anti-angiogenesis properties. Compound 16f has been identified as a potent anti-angiogenesis molecule, which can be considered as a new lead structure. The molecular docking analysis displayed the higher binding affinity of 16f with KRAS, Wnt and VEGF. Based on the earlier proven pharmacophore analogues of cancer a novel 2-(substituted-2 H -chromen-3-yl)-5-aryl-1 H -imidazoles were rationally designed, synthesized and used for competitive biological activity against cancer cell lines.