El-Gamal, Mohammed I. Jung, Myung-Ho Oh, Chang-Hyun 2024-01-20T19:03:06Z 2024-01-20T19:03:06Z 2022-01-10 2010-06-01 0960-894X https://pubs.kist.re.kr/handle/201004/131340 FMS is a type III receptor tyrosine kinase that binds to the macrophage or monocyte colony stimulating factor (M-CSF or CSF-1). Signal transduction through that binding results in survival, proliferation, and differentiation of monocyte/macrophage lineage. In this study, we report the discovery of a new potent inhibitor of FMS kinase. The synthesized pyrrolo[3,2-c] pyridine derivative (compound 1) was initially tested at a single concentration of 1 mu M against 47 different kinases. At this concentration, the% inhibitions of the enzymatic activities of FMS and KDR kinases were 90% and 71%, respectively, while the inhibition in activity was less than 58% for all of the other kinases. For compound 1, the IC50 values against FMS and KDR were 96 and 1058 nM, respectively. So, compound 1 was found to be 11 times more selective for FMS kinase than KDR kinase. Compound 1 can be used as a promising lead for the development of new selective inhibitors of FMS kinase, which can be used as useful therapeutic tools for treatment of several inflammatory and cancer disorders. (C) 2010 Published by Elsevier Ltd. English Pergamon Press Ltd. COLONY-STIMULATING FACTOR COLLAGEN-INDUCED ARTHRITIS C-FMS BREAST-CANCER FACTOR-I ANTIINFLAMMATORY AGENTS EXPRESSION MACROPHAGES BLOCKADE RECEPTOR Discovery of a new potent bisamide FMS kinase inhibitor Article 10.1016/j.bmcl.2010.04.088 1 Bioorganic & Medicinal Chemistry Letters, v.20, no.11, pp.3216 - 3218 Bioorganic & Medicinal Chemistry Letters 20 11 3216 3218 scie scopus 000277788900004 2-s2.0-77953286131 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article COLONY-STIMULATING FACTOR COLLAGEN-INDUCED ARTHRITIS C-FMS BREAST-CANCER FACTOR-I ANTIINFLAMMATORY AGENTS EXPRESSION MACROPHAGES BLOCKADE RECEPTOR FMS KDR Tyrosine kinase Kinase inhibitor Antiinflammatory Cancer Selectivity Bisamide