Design and synthesis of aminocoumarin derivatives as DPP-IV inhibitors and anticancer agents

We have designed 3-aminocoumarin derivatives 11a–f and 7-amino-4-methylcoumarin derivatives 17a–l for DPP-IV inhibition. Compounds 17h, 17i and 17k showed moderate activity as compared to standard drug Vildagliptin. Interestingly, compound 17l showed very good anticancer activity against A549 cell line with IC50 value 24 ± 0.1 nM as compared to standard drug fluorouracil with IC50 value 11.13 ± 0.083 µM. [Display omitted] •Aminocoumarin derivatives have been synthesized and studied for their biological activities.•One of the compounds has shown 52.90% DPP-IV inhibition at 25 µM concentration.•One of the compounds has shown IC50 value 24 ± 0.1 nM against A549 lungs cancer cell line. DPP-IV “a moonlighting protein” has immerged as promising pathway to control Type 2 diabetes as well as found to play key role in earlier stages of cancer. Here we have reported design, synthesis and applications of aminocoumarin derivatives as DPP-IV inhibitors. Compounds have been synthesized and studied for their DPP-IV inhibition activity. Three compounds have shown moderate inhibition at 100 µM concentration. All compounds were also screened for their anticancer activity against A549 (Lung cancer cell line), MCF-7 (Breast cancer cell line) using MTT assay. One of the compounds has shown very good anticancer activity with IC50 value 24 ± 0.1 nM against A549 cell line.