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

Article Details

Citation

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
DrugTargetPropertyMeasurementpHTemperature (°C)
AlsterpaulloneCyclin-dependent kinase 1IC 50 (nM)35N/AN/ADetails
AlsterpaulloneGlycogen synthase kinase-3 betaIC 50 (nM)4N/AN/ADetails