Synthesis and SAR of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as novel, selective c-Jun N-terminal kinase inhibitors |
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| Authors: | 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 |
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| Institution: | Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA. mei.liu@abbott.com |
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| Abstract: | A novel class of 1,9-dihydro-9-hydroxypyrazolo3,4-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. |
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