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Synthesis and sar of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors

Academic Article
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Overview

authors

  • Shin, Y. S.
  • Chen, W. M.
  • Habel, J.
  • Duckett, Derek
  • Ling, Y. Y.
  • Koenig, M.
  • He, Y.
  • Vojkovsky, T.
  • LoGrasso, Philip
  • Kamenecka, Theodore

publication date

  • June 2009

journal

  • Bioorganic & Medicinal Chemistry Letters  Journal

abstract

  • A novel series of c-jun N-terminal kinase (JNK) inhibitors were designed and developed from a high-throughput-screening hit. Through the optimization of the piperazine amide 1, several potent compounds were discovered. The X-ray crystal structure of 4g showed a unique binding mode different from other well known JNK3 inhibitors.

subject areas

  • Amides
  • Crystallography, X-Ray
  • Drug Evaluation, Preclinical
  • Humans
  • JNK Mitogen-Activated Protein Kinases
  • Piperazines
  • Protein Binding
  • Protein Kinase Inhibitors
  • Structure-Activity Relationship
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Research

keywords

  • JNK
  • Kinase
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Identity

PubMed Central ID

  • PMC2737472

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2009.03.086

PubMed ID

  • 19433357
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Additional Document Info

start page

  • 3344

end page

  • 3347

volume

  • 19

issue

  • 12

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