Pyrrolo[3,2-c]pyridine derivatives with potential inhibitory effect against FMS kinase: in vitro biological studies
- Pyrrolo[3,2-c]pyridine derivatives with potential inhibitory effect against FMS kinase: in vitro biological studies
- 오창현; 모하메드 엘 가말
- CSF-1R; kinase inhibitor; FMS; pyrrolo[3,2-c]pyridine
- Issue Date
- Journal of enzyme inhibition and medicinal chemistry
- VOL 33, NO 1-1166
- A series of eighteen pyrrolo[3,2-c]pyridine derivatives were tested for inhibitory effect against FMS kinase. Compounds 1e and 1r were the most potent among all the other tested analogues (IC50  =  60  nM and 30  nM, respectively). They were 1.6 and 3.2 times, respectively, more potent than our lead compound, KIST101029 (IC50  96  nM). Compound 1r was tested over a panel of 40 kinases including FMS, and exerted selectivity against FMS kinase. It was further tested against bone marrow-derived macrophages (BMDM) and its IC50 was 84  nM (2.32-fold more potent than KIST101029 (IC50  195  nM)). Compound 1r was also tested for antiproliferative activity against a panel of six ovarian, two prostate, and five breast cancer cell lines, and its IC50 values ranged from 0.15-1.78  µ M. It possesses also the merit of selectivity towards cancer cells than normal fibroblasts.
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