2. Academic Validation
  3. Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH)

Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH)

  • Eur J Med Chem. 2010 Jan;45(1):335-42. doi: 10.1016/j.ejmech.2009.10.018.
Anja Becker 1,  Simone Kohfeld,  Annette Lader,  Lutz Preu,  Tanja Pies,  Karen Wieking,  Yoan Ferandin,  Marie Knockaert,  Laurent Meijer,  Conrad Kunick
Affiliations

Affiliation

  • 1 Technische Universität Braunschweig, Institut für Pharmazeutische Chemie, Beethovenstrasse 55, D-38106 Braunschweig, Germany.
PMID: 19906467 DOI: 10.1016/j.ejmech.2009.10.018
Abstract

A collection of paullones was tested for inhibitory activity against mitochondrial malate dehydrogenase (mMDH) as a biological target for antiproliferative activity. Based on the results of this screening, 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters were developed as selective mMDH inhibitors. The new derivatives did not show noteworthy antiproliferative activity when tested on a panel of Cancer cell lines, suggesting that mMDH inhibition is of minor relevance for the growth inhibition caused by paullones.

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