Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH).
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Becker A, Kohfeld S, Lader A, Preu L, Pies T, Wieking K, Ferandin Y, Knockaert M, Meijer L, Kunick C
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. Epub 2009 Oct 14.
- PubMed ID
- 19906467 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Alsterpaullone Cyclin-dependent kinase 1 IC 50 (nM) 35 N/A N/A Details Alsterpaullone Glycogen synthase kinase-3 beta IC 50 (nM) 4 N/A N/A Details