Design, Synthesis and Biological Evaluation of Aryl Benzimidazole-Pyridones as Cytotoxic Agents

Abstract

A new library of Aryl Benzimidazole-Pyridones (9a–j) has been synthesized, their structures were determined by ¹HNMR,¹³CNMR and mass spectral data. Further, these compounds explored for their anticancer application on four human cancer cell lines such as human prostate cancer cell line (PC3), lung cancer (A549), breast cancer (MCF-7) and human ovarian cancer (A2780) by employing MTT assay and results were compared with known anticancer agent asetoposide. All these compounds displayed remarkable cytotoxic activity. Among them, five compounds 9a, 9b, 9c, 9h and 9i displayed more potent activity. All compounds exhibited a discerning cytotoxic effect on cancer cells while not affecting normal Vero cells (IC50 = >22 µM), so providing justification for the strategic design approach employed in the development of a targeted anticancer drug.

Graphical Abstract

Keywords:

• Benzimidazole
• camptothecin
• nocodazole
• 2-pyridone and cytotoxic

Acknowledgments

The authors are thankful to Department of Chemistry, Osmania Universityfor constant encouragement in providing laboratory facilities and analytical data.

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

The authors are also grateful to the Deanship of Scientific Research, King Khalid University for the financial support [Grant No. RGP. 2/21/44].