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

Title
Cell-Based Biological Evaluation of a New Bisamide FMS Kinase Inhibitor Possessing Pyrrolo[3,2-c]pyridine Scaffold
Authors
모하메드엘가말모하메드 사미르마흐무드 가말엘딘유경호백대진오창현
Keywords
Anticancer; Bisamide; Diarylamide; FMS kinase; Pyrrolo[3,2-c]pyridine
Issue Date
2014-09
Publisher
Archiv der Pharmazie
Citation
VOL 347, NO 9, 635-641
Abstract
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.
URI
http://pubs.kist.re.kr/handle/201004/48271
ISSN
03656233
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KIST Publication > Article
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