Literature DB >> 26753914

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

Eun-Young Kim1, Seung-Tae Kang1, Heejung Jung2,3, Chi Hoon Park2,3, Chang-Soo Yun2,3, Jong Yeon Hwang2,3, Byung Jin Byun2, Chong Ock Lee2, Hyoung Rae Kim2, Jae Du Ha2, Do Hyun Ryu1, Sung Yun Cho4,5.   

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.

Entities:  

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

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Substances:

Year:  2016        PMID: 26753914     DOI: 10.1007/s12272-015-0703-7

Source DB:  PubMed          Journal:  Arch Pharm Res        ISSN: 0253-6269            Impact factor:   4.946


  2 in total

1.  Towards dual inhibitors of the MET kinase and WNT signaling pathway; design, synthesis and biological evaluation.

Authors:  Vegard Torp Lien; Margrethe Konstanse Kristiansen; Solveig Pettersen; Mads Haugland Haugen; Dag Erlend Olberg; Jo Waaler; Jo Klaveness
Journal:  RSC Adv       Date:  2019-11-13       Impact factor: 4.036

2.  A new compound of thiophenylated pyridazinone IMB5043 showing potent antitumor efficacy through ATM-Chk2 pathway.

Authors:  Jianhua Gong; Yanbo Zheng; Ying Wang; Weijin Sheng; Yi Li; Xiujun Liu; Shuyi Si; Rongguang Shao; Yongsu Zhen
Journal:  PLoS One       Date:  2018-02-02       Impact factor: 3.240

  2 in total

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