Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH)
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- 作者：Anja Becker ; Simone Kohfeld ; Annette Lader ; Lutz Preu ; Tanja Pies ; Karen Wieking ; Yoan Fer ; in ; Marie Knockaert ; Laurent Meijer ; Conrad Kunick
- 关键词：Antiproliferative activity ; Enzyme inhibition ; Mitochondrial malate dehydrogenase ; Paullone ; Kinase
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2010
- 出版时间：January 2010
- 年：2010
- 卷：45
- 期：1
- 页码：335-342
- 全文大小：292 K
文摘
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.