Synthesis and Evaluation of F-18 Labeled Pyrido[3,2-B]pyrazine Derivative as a Potential Imaging Agent for Non-Small-Cell Lung Cancer
Synthesis and Evaluation of F-18 Labeled Pyrido[3,2-B]pyrazine Derivative as a Potential Imaging Agent for Non-Small-Cell Lung Cancer
박정훈(한국원자력연구원); 김희중(동국대학교); 김동연(전남대학교); 양승대(한국원자력연구원); 허민구(한국원자력연구원); 김상욱(동국대학교); 유국현(동국대학교)
36권 7호, 1778~1783쪽
초록
Pyridopyrazine derivatives have been known as Wnt-2/β-catenin signaling pathway inhibitors. Wnt-2 overexpression may be involved in non-small-cell lung cancer (NSCLC). A novel 2-(4-[18F]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 [ 18F]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.
Abstract
Pyridopyrazine derivatives have been known as Wnt-2/β-catenin signaling pathway inhibitors. Wnt-2 overexpression may be involved in non-small-cell lung cancer (NSCLC). A novel 2-(4-[18F]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 [ 18F]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.
- 발행기관:
- 대한화학회
- 분류:
- 화학