Alkyl chain substituted 1,9-pyrazoloanthrones exhibit prominent inhibitory effect on c-Jun N-terminal kinase (JNK).
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.
Solid State and Structural Chemistry Unit, Indian Institute of Science, Bangalore, India. ssctng@sscu.iisc.ernet.in.
Karothu Durga
KD
Prasad
Jamma
J
Trinath
Ansuman
A
Biswas
Kanagaraj
K
Sekar
Kithiganahalli N
KN
Balaji
Tayur N
TN
Guru Row
D000478:Alkylation; D000818:Animals; D000873:Anthracenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D020134:Catalytic Domain; D016923:Cell Death / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D018360:Crystallography, X-Ray; D048031:JNK Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008070:Lipopolysaccharides / Q000494:pharmacology; D017737:Macrophages, Peritoneal / Q000187:drug effects; D008810:Mice, Inbred C57BL; D008968:Molecular Conformation; D010766:Phosphorylation / Q000187:drug effects; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013816:Thermodynamics; D014584:User-Computer Interface
D000873:Anthracenes; D008070:Lipopolysaccharides; D047428:Protein Kinase Inhibitors; D048031:JNK Mitogen-Activated Protein Kinases