Source:http://linkedlifedata.com/resource/pubmed/id/18652444
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
16
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pubmed:dateCreated |
2008-8-22
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pubmed:abstractText |
Synthesis of novel nonfused amidino-substituted thienyl- and furylvinylbenzimidazole: derivatives and their photochemical cyclization into corresponding diazacyclopenta[ c]fluorenes is described. All studied compounds showed prominent growth inhibitory effect. The fused compounds showed stronger activity than nonfused ones, whereby imidazolyl-substituted compound 11 proved to be the most active one. Besides, it induced strong G2/M arrest of the cell cycle followed by drastic apoptosis, which is in accordance with the DNA intercalative binding mode determined by the spectroscopic studies. Nonfused derivatives induced strong S phase arrest of the cell cycle followed by apoptosis that together with DNA minor groove binding mode pointed to topoisomerase I inhibition. In addition, all nonfused compounds revealed pronounced selectivity toward tumor cells in comparison with nontumor cells. On the basis of the presented results, both nonfused and fused thiophene-containing imidazolyl derivatives should be considered as promising lead compounds for further investigation.
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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/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Benzimidazoles,
http://linkedlifedata.com/resource/pubmed/chemical/DNA,
http://linkedlifedata.com/resource/pubmed/chemical/DNA Topoisomerases, Type I,
http://linkedlifedata.com/resource/pubmed/chemical/Fluorenes,
http://linkedlifedata.com/resource/pubmed/chemical/RNA
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
1520-4804
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pubmed:author | |
pubmed:issnType |
Electronic
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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 |
4899-910
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pubmed:meshHeading |
pubmed-meshheading:18652444-Antineoplastic Agents,
pubmed-meshheading:18652444-Apoptosis,
pubmed-meshheading:18652444-Benzimidazoles,
pubmed-meshheading:18652444-Cell Line, Tumor,
pubmed-meshheading:18652444-Circular Dichroism,
pubmed-meshheading:18652444-DNA,
pubmed-meshheading:18652444-DNA Topoisomerases, Type I,
pubmed-meshheading:18652444-Fluorenes,
pubmed-meshheading:18652444-Humans,
pubmed-meshheading:18652444-Nucleic Acid Denaturation,
pubmed-meshheading:18652444-Photochemistry,
pubmed-meshheading:18652444-RNA,
pubmed-meshheading:18652444-Spectrophotometry, Ultraviolet
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pubmed:year |
2008
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pubmed:articleTitle |
Novel amidino-substituted thienyl- and furylvinylbenzimidazole: derivatives and their photochemical conversion into corresponding diazacyclopenta[c]fluorenes. synthesis, interactions with DNA and RNA, and antitumor evaluation. 4.
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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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