Section 53
Chapter 52,551

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

Becker, A.; Kohfeld, S.; Lader, A.; Preu, L.; Pies, T.; Wieking, K.; Ferandin, Y.; Knockaert, M.; Meijer, L.; Kunick, C.

European Journal of Medicinal Chemistry 45(1): 335-342


ISSN/ISBN: 1768-3254
PMID: 19906467
DOI: 10.1016/j.ejmech.2009.10.018
Accession: 052550055

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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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