Synthesis and biological activity of new 4-(Pyridin-4-yl)-(3-methoxy-5- methylphenyl)- 1H-pyrazoles derivatives as ROS Receptor tyrosine kinase inhibitors

Byung Sun Park, Ibrahim M. El-deeb, Kyung Ho Yoo, Dong Keun Han, Jin Sung Tae, So Ha Lee

Research output: Contribution to journalArticle

6 Citations (Scopus)

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 IC50 value of 6.25 μM. 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.

Original languageEnglish
Pages (from-to)3629-3634
Number of pages6
JournalBulletin of the Korean Chemical Society
Volume33
Issue number11
DOIs
Publication statusPublished - 2012 Nov 20

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Pyrazoles
Lead compounds
Receptor Protein-Tyrosine Kinases
Bioactivity
Hydrogen bonds
Phosphotransferases
Derivatives
pyridine
pyrazole
acetonitrile

All Science Journal Classification (ASJC) codes

  • Chemistry(all)

Cite this

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title = "Synthesis and biological activity of new 4-(Pyridin-4-yl)-(3-methoxy-5- methylphenyl)- 1H-pyrazoles derivatives as ROS Receptor tyrosine kinase inhibitors",
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 IC50 value of 6.25 μM. 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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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; El-deeb, Ibrahim M.; Yoo, Kyung Ho; Han, Dong Keun; Tae, Jin Sung; Lee, So Ha.

In: Bulletin of the Korean Chemical Society, Vol. 33, No. 11, 20.11.2012, p. 3629-3634.

Research output: Contribution to journalArticle

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AU - El-deeb, Ibrahim M.

AU - Yoo, Kyung Ho

AU - Han, Dong Keun

AU - Tae, Jin Sung

AU - Lee, So Ha

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