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. 2016 Apr;39(4):453-464.
doi: 10.1007/s12272-015-0703-7. Epub 2016 Jan 11.

Discovery of substituted pyrazol-4-yl pyridazinone derivatives as novel c-Met kinase inhibitors

Eun-Young Kim  1 , Seung-Tae Kang  1 , Heejung Jung  2   3 , Chi Hoon Park  2   3 , Chang-Soo Yun  2   3 , Jong Yeon Hwang  2   3 , Byung Jin Byun  2 , Chong Ock Lee  2 , Hyoung Rae Kim  2 , Jae Du Ha  2 , Do Hyun Ryu  1 , Sung Yun Cho  4   5
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Discovery of substituted pyrazol-4-yl pyridazinone derivatives as novel c-Met kinase inhibitors

Eun-Young Kim et al. Arch Pharm Res. 2016 Apr.

Abstract

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.

Keywords: Kinase inhibitor; Mesenchymal epithelial transition factor; Pyridazine derivatives; c-MET inhibitor.

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