Source:http://linkedlifedata.com/resource/pubmed/id/20471844
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
12
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pubmed:dateCreated |
2010-6-23
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pubmed:abstractText |
Phenazine 5,10-dioxides are prodrugs for antitumor therapy that undergo hypoxic-selective bioreduction to form cytotoxic species. Here we investigate the expanded system benzo[a]phenazine 7,12-dioxides as selective hypoxic cytotoxin-scaffold. The clonogenic survival of V79 cells on aerobic and anaerobic conditions, conduct us to study antiproliferative activity on Caco-2 tumoral cells in normoxia. Electrochemical, DNA-interaction and DNA-damage studies were performed to establish the mode of action. The results demonstrated the potential biological properties of the studied scaffold being derivatives 6-10 structural hits for further chemical-modifications to become into therapeutics for solid tumors. Compounds 6 and 8 with cytotoxicity against V79 cells in both conditions (aerobia and anaerobia) were also cytotoxic against Caco-2 tumoral cells in aerobiosis.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
1464-3391
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pubmed:author |
pubmed-author:AravenaMaría de Los AngelesMde L,
pubmed-author:BrunoAna MaríaAM,
pubmed-author:CabreraMauricioM,
pubmed-author:CascanteMartaM,
pubmed-author:CerecettoHugoH,
pubmed-author:GonzálezMercedesM,
pubmed-author:López de CeráinAdelaA,
pubmed-author:LavaggiMaría LauraML,
pubmed-author:MongeAntonioA,
pubmed-author:Olea-AzarClaudioC,
pubmed-author:PachónGiselaG,
pubmed-author:PietrasantaLía ILI
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pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4433-40
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pubmed:meshHeading |
pubmed-meshheading:20471844-Animals,
pubmed-meshheading:20471844-Antineoplastic Agents,
pubmed-meshheading:20471844-Caco-2 Cells,
pubmed-meshheading:20471844-Cell Hypoxia,
pubmed-meshheading:20471844-Cell Line,
pubmed-meshheading:20471844-Colonic Neoplasms,
pubmed-meshheading:20471844-Cricetinae,
pubmed-meshheading:20471844-DNA Damage,
pubmed-meshheading:20471844-DNA Fragmentation,
pubmed-meshheading:20471844-Humans,
pubmed-meshheading:20471844-Phenazines
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pubmed:year |
2010
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pubmed:articleTitle |
Study of benzo[a]phenazine 7,12-dioxide as selective hypoxic cytotoxin-scaffold. Identification of aerobic-antitumoral activity through DNA fragmentation.
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pubmed:affiliation |
Laboratorio de Química Orgánica, Facultad de Ciencias-Facultad de Química, Universidad de la República, 11400 Montevideo, Uruguay.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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