Journal
BULLETIN OF THE KOREAN CHEMICAL SOCIETY
Volume 33, Issue 5, Pages 1571-1576Publisher
KOREAN CHEMICAL SOC
DOI: 10.5012/bkcs.2012.33.5.1571
Keywords
Anticancer; Diarylurea; Multiple-kinase; Pyrrolo[3,2-c]pyridine
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Funding
- Korea Institute of Science and Technology (KIST) [2E22360]
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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 mu M 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 mu M 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.
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