| Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH). | |
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MedLine Citation:
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PMID: 19906467 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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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Authors:
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Anja Becker; Simone Kohfeld; Annette Lader; Lutz Preu; Tanja Pies; Karen Wieking; Yoan Ferandin; Marie Knockaert; Laurent Meijer; Conrad Kunick |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2009-10-14 |
Journal Detail:
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Title: European journal of medicinal chemistry Volume: 45 ISSN: 1768-3254 ISO Abbreviation: Eur J Med Chem Publication Date: 2010 Jan |
Date Detail:
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Created Date: 2010-02-01 Completed Date: 2010-04-29 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0420510 Medline TA: Eur J Med Chem Country: France |
Other Details:
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Languages: eng Pagination: 335-42 Citation Subset: IM |
Copyright Information:
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Copyright 2009 Elsevier Masson SAS. All rights reserved. |
Affiliation:
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Technische Universit?t Braunschweig, Institut f?r Pharmazeutische Chemie, Beethovenstrasse 55, D-38106 Braunschweig, Germany. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Benzazepines
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chemical synthesis*,
chemistry,
pharmacology* Carboxylic Acids / chemistry* Cell Line, Tumor Drug Discovery* Enzyme Inhibitors / chemical synthesis, chemistry, pharmacology Humans Inhibitory Concentration 50 Malate Dehydrogenase / antagonists & inhibitors* Mitochondria / enzymology* Substrate Specificity |
| Chemical | |
Reg. No./Substance:
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0/Benzazepines; 0/Carboxylic Acids; 0/Enzyme Inhibitors; 0/paullone; EC 1.1.1.37/Malate Dehydrogenase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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