Design and synthesis of an anticancer diarylurea derivative with multiple-kinase inhibitory effect

Title
Design and synthesis of an anticancer diarylurea derivative with multiple-kinase inhibitory effect
Authors
모하메드엘가말오창현
Keywords
Anticancer; Diarylurea; Multiple-kinase; Pyrrolo[3,2-c]pyridine
Issue Date
2012-05
Publisher
Bulletin of the Korean Chemical Society
Citation
VOL 33, NO 5, 1571-1576
Abstract
A diarylurea compound 1 possessing pyrrolo[3,2-c]pyridine nucleus was designed and synthesized with structure similarity to Sorafenib. Compound 1 was tested over 60-cancer cell line panel at a single dose concentration of 10 μM and showed high activity. It was further tested in a five-dose mode to determine its IC50, TGI, and LC50 values over the 60 cell lines. Compound 1 showed high potency and good efficacy, and was accordingly tested at a single dose concentration of 10 μM over a panel of 40 kinases. At this concentration, it completely inhibited the enzymatic activities of a number of oncogenic kinases, including ABL, ALK, c-RAF, FLT3, KDR, and TrkB. The target compound was subsequently tested over these 6 kinases in 10-dose testing mode in order to determine its IC50 values.
URI
http://pubs.kist.re.kr/handle/201004/45708
ISSN
02532964
Appears in Collections:
KIST Publication > Article
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