Discovery of a new potent bisamide FMS kinase inhibitor

Title
Discovery of a new potent bisamide FMS kinase inhibitor
Authors
엘가말정명호오창현
Keywords
FMS; KDR; Tyrosine kinase; Kinase inhibitor; Antiinflammatory; Cancer; Selectivity; Bisamide
Issue Date
2010-06
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 20, NO 11, 3216-3218
Abstract
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 μM 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.
URI
http://pubs.kist.re.kr/handle/201004/38265
ISSN
0960-894X
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