Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Synthesis and Biological Activity of New 4-(Pyridin-4-yl)-(3-methoxy-5-methylphenyl)-1H-pyrazoles Derivatives as ROS Receptor Tyrosine Kinase Inhibitors

  • Park, Byung Sun (Department of Chemistry, Yonsei University) ;
  • El-Deeb, Ibrahim M. (Institute for Glycomics, Griffith University, Gold Coast Campus) ;
  • Yoo, Kyung Ho (Chemical Kinomics Research Center, Korea Institute of Science and Technology) ;
  • Han, Dong Keun (Center for Biomaterials, Korea Institute of Science and Technology) ;
  • Tae, Jin Sung (Department of Chemistry, Yonsei University) ;
  • Lee, So Ha (Chemical Kinomics Research Center, Korea Institute of Science and Technology)
  • Received : 2012.07.22
  • Accepted : 2012.08.08
  • Published : 2012.11.20
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Abstract

A series of new 4-(pyridin-4-yl)-(3-methoxy-5-methylphenyl)-1H-pyrazoles (6a-k & 7a-l) has been rationally designed based on the structure of the lead compound KIST301080, a selective ROS receptor tyrosine kinase inhibitor, in order to study the activity of ROS of this new class of inhibitors. The compounds were synthesized and screened against ROS kinase, where compound 6h showed moderate inhibitory activity with an $IC_{50}$ value of $6.25{\mu}M$. The study emphasized the importance of the acetonitrile group at the pyrazole ring and also the importance of having a hydrogen bond donor on the distal phenyl ring linked to the pyridine moiety.

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References

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