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KMID : 0043320160390040453
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Archives of Pharmacal Research
2016 Volume.39 No. 4 p.453 ~ p.464
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Discovery of substituted pyrazol-4-yl pyridazinone derivatives as novel c-Met kinase inhibitors
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Kim Eun-Young
Kang Seung-Tae
Jung Hee-Jung
Park Chi-Hoon
Yun Chang-Soo
Hwang Jong-Yeon
Byun Byung-Jin
Lee Chong-Ock
Kim Hyoung-Rae
Ha Jae-Du
Ryu Do-Hyun
Cho Sung-Yun
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Abstract
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A series of pyridazin-3-one substituted with morpholino-pyrimidine derivatives was synthesized and evaluated as tyrosine kinase inhibitors against c-Met enzyme, and anti-proliferative activities of Hs746T human gastric cancer cell line. Most of compounds exhibited good biological activity, while compound 10, 12a, 14a displayed excellent c-Met enzyme inhibitory activities and Hs746T cell-based activities.
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KEYWORD
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Mesenchymal epithelial transition factor, c-MET inhibitor, Pyridazine derivatives, Kinase inhibitor
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