Design and synthesis of an anticancer diarylurea derivative with multiple-kinase inhibitory effect
- Design and synthesis of an anticancer diarylurea derivative with multiple-kinase inhibitory effect
- 모하메드엘가말; 오창현
- Anticancer; Diarylurea; Multiple-kinase; Pyrrolo[3,2-c]pyridine
- Issue Date
- Bulletin of the Korean Chemical Society
- VOL 33, NO 5, 1571-1576
- 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.
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