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

  • Org Biomol Chem. 2014 Jul 14;12(26):4656-62. doi: 10.1039/c4ob00548a.
Karothu Durga Prasad  1 ,  Jamma Trinath ,  Ansuman Biswas ,  Kanagaraj Sekar ,  Kithiganahalli N Balaji ,  Tayur N Guru Row
Affiliations
  • 1. Solid State and Structural Chemistry Unit, Indian Institute of Science, Bangalore, India. [email protected].
PMID: 24853961 DOI: 10.1039/c4ob00548a
Abstract

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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