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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
12
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pubmed:dateCreated |
2008-12-3
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pubmed:abstractText |
A series of amidino-substituted benzimidazoles, related to furyl-phenyl- and thienyl-phenyl-acrylates, naphthofurans and naphthothiophenes were prepared, their antitumor evaluation and interactions with ct-DNA have been investigated. All tested compounds show differential and strong antitumor activity without apparent difference depending on their structures. Interestingly, the MCF-7 tumor cell line is highly sensitive to all compounds. Compounds 6-9 showed noticeable selectivity in regard to normal fibroblasts (WI 38). Compounds 4-9 interact with ct-DNA by more binding modes, whose mutual distribution is dependent on the compound/DNA ratio. The "acyclic"4-6 and "cyclic" compound 7 interact mostly within the minor groove of DNA, although partial intercalation of 6 and 7 cannot be excluded. The "cyclic" compounds 8 and 9 intercalate between DNA base pairs at high excess of DNA over compounds.
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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 |
Dec
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pubmed:issn |
1768-3254
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:volume |
43
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2877-90
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pubmed:meshHeading |
pubmed-meshheading:18395297-Acrylates,
pubmed-meshheading:18395297-Antineoplastic Agents,
pubmed-meshheading:18395297-Benzimidazoles,
pubmed-meshheading:18395297-Binding Sites,
pubmed-meshheading:18395297-Cell Line, Tumor,
pubmed-meshheading:18395297-Cell Proliferation,
pubmed-meshheading:18395297-Circular Dichroism,
pubmed-meshheading:18395297-DNA,
pubmed-meshheading:18395297-Dose-Response Relationship, Drug,
pubmed-meshheading:18395297-Drug Screening Assays, Antitumor,
pubmed-meshheading:18395297-Furans,
pubmed-meshheading:18395297-HeLa Cells,
pubmed-meshheading:18395297-Humans,
pubmed-meshheading:18395297-Molecular Structure,
pubmed-meshheading:18395297-Spectrophotometry, Ultraviolet,
pubmed-meshheading:18395297-Stereoisomerism,
pubmed-meshheading:18395297-Structure-Activity Relationship,
pubmed-meshheading:18395297-Temperature,
pubmed-meshheading:18395297-Thiophenes
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pubmed:year |
2008
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pubmed:articleTitle |
Synthesis, antitumor evaluation and DNA binding studies of novel amidino-benzimidazolyl substituted derivatives of furyl-phenyl- and thienyl-phenyl-acrylates, naphthofurans and naphthothiophenes.
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pubmed:affiliation |
Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Maruli?ev trg 20, P.O. Box 177, HR-10000 Zagreb, Croatia.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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