Document Detail


Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH).
MedLine Citation:
PMID:  19906467     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
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:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2009-10-14
Journal Detail:
Title:  European journal of medicinal chemistry     Volume:  45     ISSN:  1768-3254     ISO Abbreviation:  Eur J Med Chem     Publication Date:  2010 Jan 
Date Detail:
Created Date:  2010-02-01     Completed Date:  2010-04-29     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0420510     Medline TA:  Eur J Med Chem     Country:  France    
Other Details:
Languages:  eng     Pagination:  335-42     Citation Subset:  IM    
Copyright Information:
Copyright 2009 Elsevier Masson SAS. All rights reserved.
Affiliation:
Technische Universit?t Braunschweig, Institut f?r Pharmazeutische Chemie, Beethovenstrasse 55, D-38106 Braunschweig, Germany.
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MeSH Terms
Descriptor/Qualifier:
Benzazepines / 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:
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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