title: Discovery of substituted pyrazol-4-yl pyridazinone derivatives as novel c-Met kinase inhibitors.
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.
authors.affiliation: Department of Chemistry, Sungkyunkwan University, Suwon, 440-746, Korea.
authors.forename: Eun-Young
authors.initials: EY
authors.lastname: Kim
authors.affiliation: Department of Chemistry, Sungkyunkwan University, Suwon, 440-746, Korea.
authors.forename: Seung-Tae
authors.initials: ST
authors.lastname: Kang
authors.affiliation: Korea Research Institute of Chemical Technology, PO Box 107, Daejeon, 305-600, Korea.|Department of Medicinal and Pharmaceutical Chemistry, University of Science and Technology, Daejeon, 305-550, Korea.
authors.forename: Heejung
authors.initials: H
authors.lastname: Jung
authors.affiliation: Korea Research Institute of Chemical Technology, PO Box 107, Daejeon, 305-600, Korea.|Department of Medicinal and Pharmaceutical Chemistry, University of Science and Technology, Daejeon, 305-550, Korea.
authors.forename: Chi Hoon
authors.initials: CH
authors.lastname: Park
authors.affiliation: Korea Research Institute of Chemical Technology, PO Box 107, Daejeon, 305-600, Korea.|Department of Medicinal and Pharmaceutical Chemistry, University of Science and Technology, Daejeon, 305-550, Korea.
authors.forename: Chang-Soo
authors.initials: CS
authors.lastname: Yun
authors.affiliation: Korea Research Institute of Chemical Technology, PO Box 107, Daejeon, 305-600, Korea.|Department of Medicinal and Pharmaceutical Chemistry, University of Science and Technology, Daejeon, 305-550, Korea.
authors.forename: Jong Yeon
authors.initials: JY
authors.lastname: Hwang
authors.affiliation: Korea Research Institute of Chemical Technology, PO Box 107, Daejeon, 305-600, Korea.
authors.forename: Byung Jin
authors.initials: BJ
authors.lastname: Byun
authors.affiliation: Korea Research Institute of Chemical Technology, PO Box 107, Daejeon, 305-600, Korea.
authors.forename: Chong Ock
authors.initials: CO
authors.lastname: Lee
authors.affiliation: Korea Research Institute of Chemical Technology, PO Box 107, Daejeon, 305-600, Korea.
authors.forename: Hyoung Rae
authors.initials: HR
authors.lastname: Kim
authors.affiliation: Korea Research Institute of Chemical Technology, PO Box 107, Daejeon, 305-600, Korea.
authors.forename: Jae Du
authors.initials: JD
authors.lastname: Ha
authors.affiliation: Department of Chemistry, Sungkyunkwan University, Suwon, 440-746, Korea.
authors.forename: Do Hyun
authors.initials: DH
authors.lastname: Ryu
authors.affiliation: Korea Research Institute of Chemical Technology, PO Box 107, Daejeon, 305-600, Korea. sycho@krict.re.kr.|Department of Medicinal and Pharmaceutical Chemistry, University of Science and Technology, Daejeon, 305-550, Korea. sycho@krict.re.kr.
authors.forename: Sung Yun
authors.identifier: http://orcid.org/0000-0001-6602-605X
authors.initials: SY
authors.lastname: Cho
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D055808:Drug Discovery; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D019859:Proto-Oncogene Proteins c-met / Q000037:antagonists & inhibitors*; D011724:Pyridazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D011724:Pyridazines; D019859:Proto-Oncogene Proteins c-met
keywords: Kinase inhibitor; Mesenchymal epithelial transition factor; Pyridazine derivatives; c-MET inhibitor