4.6 Article

Alkyl chain substituted 1,9-pyrazoloanthrones exhibit prominent inhibitory effect on c-Jun N-terminal kinase (JNK)

Journal

ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 12, Issue 26, Pages 4656-4662

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c4ob00548a

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Funding

  1. Indian Institute of Science
  2. CSIR (Council of Scientific Industrial Research)
  3. DST

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N-Alkyl substituted pyrazoloanthrone derivatives were synthesized, characterized and tested for their in vitro inhibitory activity over c-Jun N-terminal kinase (JNK). Among the tested molecules, a few derivatives showed significant inhibitory activity against JNK with minimal off-target effect on other mitogen-activated protein kinase (MAP kinase) family members such as MEK1/2 and MKK3,6. These results suggested that N-alkyl (propyl and butyl) bearing pyrazoloanthrone scaffolds provide promising therapeutic inhibitors for JNK in regulating inflammation associated disorders.

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