Structural and biological evaluation of halogen derivatives of 1,9-pyrazoloanthrones towards the design of a specific potent inhibitor of c-Jun-N-terminal kinase (JNK)

Ganduri, Ramesh and Singh, Vikas and Biswas, Ansuman and Karothu, Durga Prasad and Sekar, Kanagaraj and Balaji, Kithiganahalli N and Row, Tayur N Guru (2018) Structural and biological evaluation of halogen derivatives of 1,9-pyrazoloanthrones towards the design of a specific potent inhibitor of c-Jun-N-terminal kinase (JNK). In: NEW JOURNAL OF CHEMISTRY, 42 (13). pp. 10651-10660.

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Abstract

c-Jun N-terminal kinase (JNK), a member of the MAPK family, is associated with a variety of diseases and immune responses. To dissect the mechanistic role of JNKs in such processes, a specific inhibitor for JNKs holds great value. SP600125 is a widely used inhibitor of JNKs despite its non-specific activity. In an effort to obtain better specific inhibitors, three anthrapyrazolone halogenated derivatives have been synthesized and characterized. Among the three derivatives, 5-chloro-2-(2-chloroethyl)dibenzocd,g] indazol-6(2H)-one is clearly established as a specific inhibitor of JNK with augmented expression of chemokines in LPS-activated macrophages based on modelling studies followed by in vitro and ex vivo evaluation.

Item Type:	Journal Article
Publication:	NEW JOURNAL OF CHEMISTRY
Publisher:	ROYAL SOC CHEMISTRY, THOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLAND
Additional Information:	Copyright of this article belong to ROYAL SOC CHEMISTRY, THOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLAND
Department/Centre:	Division of Biological Sciences > Microbiology & Cell Biology Division of Chemical Sciences > Solid State & Structural Chemistry Unit Others Division of Physical & Mathematical Sciences > Physics
Date Deposited:	24 Jul 2018 14:54
Last Modified:	24 Jul 2018 14:54
URI:	http://eprints.iisc.ac.in/id/eprint/60282

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