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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)

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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)dibenzo[cd,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.

Graphical abstract: 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)

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Publication details

The article was received on 19 Feb 2018, accepted on 04 May 2018 and first published on 11 May 2018


Article type: Paper
DOI: 10.1039/C8NJ00852C
Citation: New J. Chem., 2018, Advance Article
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    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)

    R. Ganduri, V. Singh, A. Biswas, D. P. Karothu, K. Sekar, K. N. Balaji and T. N. Guru Row, New J. Chem., 2018, Advance Article , DOI: 10.1039/C8NJ00852C

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