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:作为3-苄基淘水酮和普伦酮-9-羧酸烷基烷基烷基烷基烷基烷基的研制成为线粒体丙酸盐脱氢酶(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:测试酸孔的集合,用于对线粒体苹果酸脱氢酶(MMDH)的抑制活性作为抗增殖活性的生物学靶标。 基于该筛选的结果,开发了5-苄基淘水合物和普伦酮-9-羧酸烷基酯作为选择性MMDH抑制剂。 当在癌细胞系的面板上测试时,新衍生物未显示有值得注意的抗增殖活动,表明MMDH抑制对于由贫吞引起的生长抑制具有轻微相关性。

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