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Synthesis and biological evaluation of new 2-(4-fluorophenyl) imidazol-5-ones as anticancer agents

Two series of imidazolones were designed, synthesized, and evaluated for their anticancer activity against four cancer cell lines: Hela, MCF-7, PC3, and HCT-116, where four compounds 6, 25, 26, and 29 showed good potency against the whole panel. Compound 30 showed a cytotoxic effect against PC3 cell lines compared to that of the standard doxorubicin with IC50 = 8.15μM, while compounds 4 and 18 showed moderate activity with IC50 range of 10.58–11.45 μM. Enzyme inhibition assay was implemented against CDK2A and VEGFR-2; where varied activities were obtained. Compound 6 exhibited the highest inhibitory activity against VEGFR-2 with an IC50 value of 67 nM and moderate inhibition against CDK2A, while compound 26 achieved the best result against CDK2A with an IC50 value of 0.66 μM.