2. Academic Validation
  3. A class of 5-benzylidene-2-phenylthiazolinones with high potency as direct 5-lipoxygenase inhibitors

A class of 5-benzylidene-2-phenylthiazolinones with high potency as direct 5-lipoxygenase inhibitors

  • J Med Chem. 2011 Mar 24;54(6):1943-7. doi: 10.1021/jm101165z.
Bettina Hofmann 1,  Sebastian Barzen,  Carmen B Rödl,  Andreas Kiehl,  Julia Borig,  Aleksandra Zivković,  Holger Stark,  Gisbert Schneider,  Dieter Steinhilber
Affiliations

Affiliation

  • 1 Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Strasse 9, D-60438 Frankfurt, Germany. hofmann@pharmchem.uni-frankfurt.de
PMID: 21341744 DOI: 10.1021/jm101165z
Abstract

A novel class of potent direct 5-lipoxygenase (5-LO) inhibitors bearing a thiazolinone-scaffold identified by virtual screening is presented. A range of substitutions and the importance of the 2-phenyl moiety were evaluated. This series is characterized by high potency in intact polymorphonuclear leukocytes and a cell-free system, exemplified by (Z)-2-(4-chlorophenyl)-5-(4-methoxybenzylidene)-5H-thiazol-4-one (18, IC(50) = 0.28 and 0.09 μM). These disubstituted thiazolinones may possess potential for intervention with inflammatory and allergic diseases and certain Cancer types.

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