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Synthesis and SAR of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as novel, selective c-Jun N-terminal kinase inhibitors.

作者信息

Liu Mei, Xin Zhili, Clampit Jill E, Wang Sanyi, Gum Rebecca J, Haasch Deanna L, Trevillyan James M, Abad-Zapatero Cele, Fry Elizabeth H, Sham Hing L, Liu Gang

机构信息

Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA.

出版信息

Bioorg Med Chem Lett. 2006 May 15;16(10):2590-4. doi: 10.1016/j.bmcl.2006.02.046. Epub 2006 Mar 9.

DOI:10.1016/j.bmcl.2006.02.046
PMID:16527482
Abstract

A novel class of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as c-Jun-N-terminal kinase (JNK) inhibitors is described. These compounds were synthesized via the condensation of 2-nitrobenzaldehydes and hydroxypyrazoles. The structure-activity relationships (SAR) and kinase selectivity profile of the inhibitors are also discussed. Compound 16 was identified as a potent JNK inhibitor with good cellular potency.

摘要

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