Discovery of novel 2-hydroxydiarylamide derivatives as TMPRSS4 inhibitors.

TMPRSS4 is a novel type II transmembrane serine protease that has been implicated in the invasion and metastasis of colon cancer cells. In this study, a novel series of 2-hydroxydiarylamide derivatives were synthesized and evaluated for inhibiting TMPRSS4 serine protease activity and suppressing cancer cell invasion. These derivatives demonstrated good inhibitory activity against TMPRSS4 serine protease, which correlated with the promising anti-invasive activity of colon cancer cells overexpressing TMPRSS4.
AuthorsSunghyun Kang, Hye-Jin Min, Min-Seo Kang, Myung-Geun Jung, Semi Kim
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 23 Issue 6 Pg. 1748-51 (Mar 15 2013) ISSN: 1464-3405 [Electronic] England
PMID23414802 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2013 Elsevier Ltd. All rights reserved.
Chemical References
  • Amides
  • Antineoplastic Agents
  • Membrane Proteins
  • Serine Proteinase Inhibitors
  • Serine Endopeptidases
  • TMPRSS4 protein, human
  • Amides (chemistry, metabolism, toxicity)
  • Antineoplastic Agents (chemical synthesis, chemistry, therapeutic use)
  • Cell Line, Tumor
  • Cell Survival (drug effects)
  • Colonic Neoplasms (drug therapy)
  • Drug Evaluation, Preclinical
  • Humans
  • Membrane Proteins (antagonists & inhibitors, metabolism)
  • Protein Binding
  • Serine Endopeptidases (metabolism)
  • Serine Proteinase Inhibitors (chemistry, metabolism, toxicity)
  • Structure-Activity Relationship

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