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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
10
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pubmed:dateCreated |
2004-4-27
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pubmed:abstractText |
The synthesis and biological evaluation of a new series of amine-substituted 2-arylbenzimidazole-4-carboxamide inhibitors of the DNA-repair enzyme poly(ADP-ribose) polymerase-1 (PARP-1) is reported. The introduction of an amine substituent at the 2-aryl position is not detrimental to activity, with most inhibitors exhibiting K(i) values for PARP-1 inhibition in the low nanomolar range. Two compounds in this series were found to potentiate the cytotoxicity of the DNA-methylating agent temozolomide by 4-5-fold in a human colorectal cancer cell line.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:CurtinNicola JNJ,
pubmed-author:EastmanBrian WBW,
pubmed-author:GoldingBernard TBT,
pubmed-author:GriffinRoger JRJ,
pubmed-author:HostomskyZdenekZ,
pubmed-author:KyleSuzanneS,
pubmed-author:LiJiankeJ,
pubmed-author:MaegleyKaren AKA,
pubmed-author:SkalitzkyDonald JDJ,
pubmed-author:WebberStephen ESE,
pubmed-author:WhiteAlex WAW,
pubmed-author:YuXiao-HongXH
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pubmed:issnType |
Print
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pubmed:day |
17
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|
pubmed:volume |
14
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2433-7
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:15109627-Amides,
pubmed-meshheading:15109627-Animals,
pubmed-meshheading:15109627-Antineoplastic Agents,
pubmed-meshheading:15109627-Benzimidazoles,
pubmed-meshheading:15109627-Cell Line, Tumor,
pubmed-meshheading:15109627-Cell Proliferation,
pubmed-meshheading:15109627-Colorectal Neoplasms,
pubmed-meshheading:15109627-Dacarbazine,
pubmed-meshheading:15109627-Drug Synergism,
pubmed-meshheading:15109627-Humans,
pubmed-meshheading:15109627-Lung Neoplasms,
pubmed-meshheading:15109627-Poly(ADP-ribose) Polymerases,
pubmed-meshheading:15109627-Structure-Activity Relationship
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pubmed:year |
2004
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pubmed:articleTitle |
Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors.
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pubmed:affiliation |
Northern Institute for Cancer Research, School of Natural Sciences-Chemistry, Bedson Building, University of Newcastle, Newcastle Upon Tyne NE1 7RU, UK.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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