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[Display omitted] • Two series of cyclic amine-containing benzimidazole carboxamide derivatives were designed and synthesized as potent anticancer agents. Most of them exhibited potent PARP1/2 inhibitory activity and in vitro antitumor activity. • 2-(1-(4,4-difluorocyclohexyl)piperidin-4-yl)-1H-benzo[ d ]imidazole-4-carboxamide (17d) could significantly inhibit PARP1/2 enzymes. • 17d also possessed obvious selective antineoplastic activity and noteworthy microsomal metabolic stability. • Further studies revealed that 17d was endowed with an excellent ADME profile. • The findings highlighted the potential of these derivatives as new anticancer agents and 17d as a candidate for the treatment of cancer. In this work, two series of cyclic amine-containing benzimidazole carboxamide derivatives were designed and synthesized as potent anticancer agents. PARP1/2 inhibitory activity assays indicated that most of the compounds showed significant activity. The in vitro antiproliferative activity of these compounds was investigated against four human cancer cell lines (MDA-MB-436, MDA-MB-231, MCF-7 and CAPAN-1), and several compounds exhibited strong cytotoxicity to tumor cells. Among them, 2-(1-(4,4-difluorocyclohexyl)piperidin-4-yl)-1H-benzo[ d ]imidazole-4-carboxamide (17d) was found to be effective PARP1/2 inhibitors (IC 50 = 4.30 and 1.58 nM, respectively). In addition, 17d possessed obvious selective antineoplastic activity and noteworthy microsomal metabolic stability. What's more, further studies revealed that 17d was endowed with an excellent ADME profile. These combined results indicated that 17d could be a promising candidate for the treatment of cancer. [ABSTRACT FROM AUTHOR]