Synthesis and biological evaluation of novel 2,3-dihydrochromeno[3,4-d]imidazol-4(1H)-one derivatives as potent anticancer cell proliferation and migration agents

• We have found a novel scaffold with better potency as antitumor agents.
• Target compound 35 could arrest G0/G1 cell-cycle and induce apoptosis of SW620 cells in a dose-dependent manner.
• 35 blocked MCF-7 cancer cell migration with low toxicity to normal LO2 cells.
• 35 inhibited tumor growth by 52.96% at 80 mg/kg/48 h for 20 days.

In this study, a series of novel molecules containing chromeno [3,4-d] imidazol-4(1H)-one was synthesized and their biological activities were evaluated. Among them, compound 35 showed a dramatic anticancer activity against HCT116 and MCF-7, and the flow cytometry assays demonstrated that it could arrest G0/G1 cell-cycle and induce apoptosis of SW620 cells in a dose-dependent manner. Besides, it also blocked MCF-7 cancer cell migration. Moreover, it inhibited tumor growth in HCT116 subcutaneously implanted xenografted mice. Taken together, compound 35 may be a promising candidate for anti-cancer agent as well as metastatic one.

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