Evaluation of novel coumarin-proline sulfonamide hybrids as anticancer and antidiabetic agents

Abstract

Cancer and diabetes are considered as two major diseases affecting human health worldwide. Various therapies are available for treatment of cancer and diabetes individually, peptide linkage containing proline sulfonamide can be a promising therapy for treatment of both cancer as well as diabetes. Here, we report design and synthesis of novel coumarin-proline sulfonamide derivatives as anticancer and antidiabetic agents. All the synthesized compounds were screened for their anticancer activity against lungs cancer cell line (A549) and breast cancer cell line (MCF7) using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide dye (MTT)assay and antidiabetic activity using DPP-IV inhibition assay. Compound 16b showed excellent activity against breast cancer cell line (MCF7) with IC₅₀ value of 1.07 µM. All compounds showed moderate DPP-IV inhibition.

Graphical Abstract

Keywords:

• Aminocoumarin
• anticancer
• DPP-IV inhibitor
• proline
• sulfonamide

Acknowledgements

Authors are thankful to The Head, Department of Chemistry, Faculty of Science, The M. S. University of Baroda for providing laboratory facilities, Department of Zoology for screening compounds for anticancer activity and Zydus Research Center, Ahmedabad, for the ESI-MS analyses and antidiabetic activity. DST purse, M.S University of Baroda for single crystal analyses.