Source:http://linkedlifedata.com/resource/pubmed/id/18232651
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
2008-2-21
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pubmed:abstractText |
The good results obtained as potential antitumor drugs with aza-anthracenediones and aza-anthrapyrazoles, e.g. pixantrone, 1a, and 1b (Chart 1), prompted us to design and synthesize a series of symmetrical bis derivatives, compounds 7-10 (Chart 1). These compounds are dimers of different aza-anthracenedione and aza-anthrapyrazolone monomers connected by the linker found to be the most appropriate among potential bis intercalators synthesized by us. The DNA-binding properties of bis derivatives 7 and 8 have been examined using fluorometric techniques: these target compounds are excellent DNA ligands, with a clear binding site preference for AT-rich duplexes. In vitro cytotoxic activity of all target compounds 7-10 and of reference compound pixantrone toward human cancer adenocarcinoma cell line HT29 is also described. Two selected compounds have been investigated for their capacity of inducing early apoptosis.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Anthracenes,
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Aza Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/DNA,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrazoles,
http://linkedlifedata.com/resource/pubmed/chemical/RNA, Messenger
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
28
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pubmed:volume |
51
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
997-1006
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pubmed:meshHeading |
pubmed-meshheading:18232651-Anthracenes,
pubmed-meshheading:18232651-Antineoplastic Agents,
pubmed-meshheading:18232651-Apoptosis,
pubmed-meshheading:18232651-Aza Compounds,
pubmed-meshheading:18232651-DNA,
pubmed-meshheading:18232651-Drug Screening Assays, Antitumor,
pubmed-meshheading:18232651-Gene Expression Profiling,
pubmed-meshheading:18232651-HT29 Cells,
pubmed-meshheading:18232651-Humans,
pubmed-meshheading:18232651-Pyrazoles,
pubmed-meshheading:18232651-RNA, Messenger
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pubmed:year |
2008
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pubmed:articleTitle |
Synthesis and antitumor evaluation of bis aza-anthracene-9,10-diones and bis aza-anthrapyrazole-6-ones.
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pubmed:affiliation |
Department of Chemical Sciences, University of Camerino, Via S. Agostino 1, 62032 Camerino, Italy. ippolito.antonini@unicam.it
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pubmed:publicationType |
Journal Article
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