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Archives of Pharmacal Research

, Volume 39, Issue 4, pp 453–464 | Cite as

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

  • Eun-Young Kim
  • Seung-Tae Kang
  • Heejung Jung
  • Chi Hoon Park
  • Chang-Soo Yun
  • Jong Yeon Hwang
  • Byung Jin Byun
  • Chong Ock Lee
  • Hyoung Rae Kim
  • Jae Du Ha
  • Do Hyun Ryu
  • Sung Yun ChoEmail author
Research Article

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

Mesenchymal epithelial transition factor c-MET inhibitor Pyridazine derivatives Kinase inhibitor 

Notes

Acknowledgments

This work was supported by a grant from the Korea Research Institute of Chemical Technology (KRICT) and the National Research Foundation of Korea (H.R.K, NRF-2012M3A9A9054902).

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Copyright information

© The Pharmaceutical Society of Korea 2016

Authors and Affiliations

  • Eun-Young Kim
    • 2
  • Seung-Tae Kang
    • 2
  • Heejung Jung
    • 1
    • 3
  • Chi Hoon Park
    • 1
    • 3
  • Chang-Soo Yun
    • 1
    • 3
  • Jong Yeon Hwang
    • 1
    • 3
  • Byung Jin Byun
    • 1
  • Chong Ock Lee
    • 1
  • Hyoung Rae Kim
    • 1
  • Jae Du Ha
    • 1
  • Do Hyun Ryu
    • 2
  • Sung Yun Cho
    • 1
    • 3
    Email author
  1. 1.Korea Research Institute of Chemical TechnologyDaejeonKorea
  2. 2.Department of ChemistrySungkyunkwan UniversitySuwonKorea
  3. 3.Department of Medicinal and Pharmaceutical ChemistryUniversity of Science and TechnologyDaejeonKorea

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