| pubmed-article:12569393 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:12569393 | lifeskim:mentions | umls-concept:C0431085 | lld:lifeskim |
| pubmed-article:12569393 | lifeskim:mentions | umls-concept:C0242958 | lld:lifeskim |
| pubmed-article:12569393 | lifeskim:mentions | umls-concept:C1533691 | lld:lifeskim |
| pubmed-article:12569393 | lifeskim:mentions | umls-concept:C1515655 | lld:lifeskim |
| pubmed-article:12569393 | lifeskim:mentions | umls-concept:C0672480 | lld:lifeskim |
| pubmed-article:12569393 | lifeskim:mentions | umls-concept:C0332324 | lld:lifeskim |
| pubmed-article:12569393 | pubmed:issue | 3 | lld:pubmed |
| pubmed-article:12569393 | pubmed:dateCreated | 2003-2-5 | lld:pubmed |
| pubmed-article:12569393 | pubmed:abstractText | 2-(4-Aminophenyl)benzothiazoles represent a potent and highly selective class of antitumour agent. In vitro, sensitive carcinoma cells deplete 2-(4-aminophenyl)benzothiazoles from nutrient media; cytochrome P450 1A1 activity, critical for execution of antitumour activity, and protein expression are powerfully induced. 2-(4-Amino-3-methylphenyl)benzothiazole-derived covalent binding to cytochrome P450 1A1 is reduced by glutathione, suggesting 1A1-dependent production of a reactive electrophilic species. In vitro, 2-(4-aminophenyl)benzothiazole-generated DNA adducts form in sensitive tumour cells only. At concentrations >100 nM, adducts were detected in DNA of MCF-7 cells treated with 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole (5F 203). 5F 203 (1 microM) led to the formation of one major and a number of minor adducts. However, treatment of cells with 10 microM 5F 203 resulted in the emergence of a new dominant adduct. Adducts accumulated steadily within DNA of MCF-7 cells exposed to 1 microM 5F 203 between 2 and 24 h. Concentrations of the lysylamide prodrug of 5F 203 (Phortress) > or = 100 nM generated adducts in the DNA of sensitive MCF-7 and IGROV-1 ovarian cells. At 1 microM, one major Phortress-derived DNA adduct was detected in these two sensitive phenotypes; 10 microM Phortress led to the emergence of an additional major adduct detected in the DNA of MCF-7 cells. Inherently resistant MDA-MB-435 breast carcinoma cells incurred no DNA damage upon exposure to Phortress (< or = 10 microM, 24 h). In vivo, DNA adducts accumulated within sensitive ovarian IGROV-1 and breast MCF-7 xenografts 24 h after treatment of mice with Phortress (20 mg kg(-1)). Moreover, Phortress-derived DNA adduct generation distinguished sensitive MCF-7 tumours from inherently resistant MDA-MB-435 xenografts implanted in opposite flanks of the same mouse. | lld:pubmed |
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| pubmed-article:12569393 | pubmed:language | eng | lld:pubmed |
| pubmed-article:12569393 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12569393 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:12569393 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:12569393 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:12569393 | pubmed:month | Feb | lld:pubmed |
| pubmed-article:12569393 | pubmed:issn | 0007-0920 | lld:pubmed |
| pubmed-article:12569393 | pubmed:author | pubmed-author:DoubleJ AJA | lld:pubmed |
| pubmed-article:12569393 | pubmed:author | pubmed-author:FarmerP BPB | lld:pubmed |
| pubmed-article:12569393 | pubmed:author | pubmed-author:BibbyM CMC | lld:pubmed |
| pubmed-article:12569393 | pubmed:author | pubmed-author:MartinE AEA | lld:pubmed |
| pubmed-article:12569393 | pubmed:author | pubmed-author:GaskellMM | lld:pubmed |
| pubmed-article:12569393 | pubmed:author | pubmed-author:CooperP APA | lld:pubmed |
| pubmed-article:12569393 | pubmed:author | pubmed-author:BradshawT DTD | lld:pubmed |
| pubmed-article:12569393 | pubmed:author | pubmed-author:HeydonR TRT | lld:pubmed |
| pubmed-article:12569393 | pubmed:author | pubmed-author:StevensM F... | lld:pubmed |
| pubmed-article:12569393 | pubmed:author | pubmed-author:LeongC-OCO | lld:pubmed |
| pubmed-article:12569393 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:12569393 | pubmed:day | 10 | lld:pubmed |
| pubmed-article:12569393 | pubmed:volume | 88 | lld:pubmed |
| pubmed-article:12569393 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:12569393 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:12569393 | pubmed:pagination | 470-7 | lld:pubmed |
| pubmed-article:12569393 | pubmed:dateRevised | 2009-11-18 | lld:pubmed |
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| pubmed-article:12569393 | pubmed:meshHeading | pubmed-meshheading:12569393... | lld:pubmed |
| pubmed-article:12569393 | pubmed:year | 2003 | lld:pubmed |
| pubmed-article:12569393 | pubmed:articleTitle | Antitumour 2-(4-aminophenyl)benzothiazoles generate DNA adducts in sensitive tumour cells in vitro and in vivo. | lld:pubmed |
| pubmed-article:12569393 | pubmed:affiliation | School of Pharmaceutical Sciences, University of Nottingham, UK. | lld:pubmed |
| pubmed-article:12569393 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:12569393 | pubmed:publicationType | Research Support, U.S. Gov't, P.H.S. | lld:pubmed |
| pubmed-article:12569393 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
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