期刊
BULLETIN OF THE KOREAN CHEMICAL SOCIETY
卷 36, 期 7, 页码 1778-1783出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/bkcs.10335
关键词
Wnt-2 inhibitors; Non-small-cell lung cancer; Pyridopyrazine derivatives; [F-18]fluoride; Imaging agent
资金
- Nuclear RD Program [2012 M2A2A7035, 2010-0025899]
- Converging Research Center Program through the Ministry of Science, ICT and Future Planning [2013K000339]
Pyridopyrazine derivatives have been known as Wnt-2/beta-catenin signaling pathway inhibitors. Wnt-2 overexpression may be involved in non-small-cell lung cancer (NSCLC). A novel 2-(4-[F-18]fluorobutoxy)-3-(phenylethynyl)pyrido[3,2-b]pyrazine was prepared to demonstrate the feasibility of NSCLC imaging agent by uptake of Wnt-2 protein. It was synthesized with tosylated precursor using [F-18]fluoride in radiochemical yield of 44-48%. In cellular uptake evaluation, H460 and H1299, Wnt-2 expressed cancer cell lines, showed 2.5-folds higher cellular uptake than that of MCF10A as a control.
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