Cell-Based Biological Evaluation of a New Bisamide FMS Kinase Inhibitor Possessing Pyrrolo[3,2-c]pyridine Scaffold

A bisamide compound 1 possessing the pyrrolo[3,2‐c]pyridine nucleus was synthesized and biologically evaluated. It was tested for kinase inhibitory activity over a panel of 47 kinases, and its selectivity toward the FMS kinase was accidentally discovered. Compound 1 was tested over a panel of seven ovarian, two prostate, and six breast cancer cell lines at a single dose concentration of 10 µM and showed high activity. It was further tested in a 5‐dose mode to determine its IC50 and total growth inhibition (TGI) values over the 15 cell lines. Compound 1 showed high potency on the submicromolar scale and good efficacy. The cytotoxic effect of compound 1 over peritoneal macrophages was also investigated. Compound 1 demonstrated higher selectivity against different cancer cell lines compared with HS‐27 fibroblasts. A bisamide compound (1) possessing the pyrrolo[3,2‐c]pyridine nucleus was synthesized and evaluated as kinase inhibitor, by screening a panel of 47 kinases. Compound 1 was found to possess selectivity for the FMS kinase, with inhibitory activity on the submicromolar scale. The cytotoxic effect of compound 1 was investigated on 15 cancer cell lines and on peritoneal macrophages.