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Design and Synthesis of an Anticancer Diarylurea Derivative with Multiple-Kinase Inhibitory Effect
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  • 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
저자명
El-Gamal. Mohammed I.,Oh. Chang-Hyun
간행물명
Bulletin of the Korean Chemical Society
권/호정보
2012년|33권 5호|pp.1571-1576 (6 pages)
발행정보
대한화학회
파일정보
정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

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 $IC_{50}$, TGI, and $LC_{50}$ 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 $IC_{50}$ values.