首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH).
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Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH).

机译:开发5-苄基paullones和paullone-9羧酸烷基酯作为线粒体苹果酸脱氢酶(mMDH)的选择性抑制剂。

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摘要

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.
机译:测试了一组paullones对线粒体苹果酸脱氢酶(mMDH)的抑制活性,该线粒体是抗增殖活性的生物学靶标。基于该筛选的结果,开发了5-苄基paullones和paullone-9-羧酸烷基酯作为选择性mMDH抑制剂。当在一组癌细胞系上进行测试时,新衍生物没有显示出值得注意的抗增殖活性,这表明mMDH抑制作用与paullones引起的生长抑制作用无关。

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