Source:http://linkedlifedata.com/resource/pubmed/id/17181164
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
26
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| pubmed:dateCreated |
2006-12-21
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| pubmed:abstractText |
A novel series of 9-benzylidene-naphtho[2,3-b]thiophen-4-ones and structurally related compounds were synthesized and evaluated for their ability to inhibit tubulin polymerization. The 4-hydroxy-3,5-dimethoxy-benzylidene analogue 15d was identified as a potent cytotoxic agent in an assay based on K562 leukemia cells. Antiproliferative activity of 15d and the 2,4-dimethoxy-3-hydroxy-benzylidene analogue 15e was additionally evaluated against a panel of 12 tumor cell lines, including multidrug resistant phenotypes. All resistant cell lines were sensitive to these compounds. Concentration-dependent flow cytometric studies showed that K562 cells as well as KB/HeLa cells treated by 15d were arrested in the G2/M phases of the cell cycle. Moreover, four compounds strongly inhibited tubulin polymerization with activities higher or comparable to those of the reference compounds. In competition experiments, the most active compounds strongly displaced radiolabeled colchicine from its binding site in the tubulin, showing IC50 values virtually 3- to 4-fold lower than that of colchicine.
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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/Colchicine,
http://linkedlifedata.com/resource/pubmed/chemical/Thiophenes,
http://linkedlifedata.com/resource/pubmed/chemical/Tubulin,
http://linkedlifedata.com/resource/pubmed/chemical/Tubulin Modulators
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| pubmed:status |
MEDLINE
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| pubmed:month |
Dec
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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 |
49
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| pubmed:owner |
NLM
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| pubmed:authorsComplete |
Y
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| pubmed:pagination |
7816-25
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| pubmed:meshHeading |
pubmed-meshheading:17181164-Animals,
pubmed-meshheading:17181164-Antineoplastic Agents,
pubmed-meshheading:17181164-Cell Cycle,
pubmed-meshheading:17181164-Cell Proliferation,
pubmed-meshheading:17181164-Cell Survival,
pubmed-meshheading:17181164-Colchicine,
pubmed-meshheading:17181164-Drug Resistance, Neoplasm,
pubmed-meshheading:17181164-Drug Screening Assays, Antitumor,
pubmed-meshheading:17181164-Female,
pubmed-meshheading:17181164-Flow Cytometry,
pubmed-meshheading:17181164-Humans,
pubmed-meshheading:17181164-Inhibitory Concentration 50,
pubmed-meshheading:17181164-K562 Cells,
pubmed-meshheading:17181164-Leukemia P388,
pubmed-meshheading:17181164-Mice,
pubmed-meshheading:17181164-Molecular Structure,
pubmed-meshheading:17181164-Structure-Activity Relationship,
pubmed-meshheading:17181164-Thiophenes,
pubmed-meshheading:17181164-Tubulin,
pubmed-meshheading:17181164-Tubulin Modulators,
pubmed-meshheading:17181164-Tumor Cells, Cultured
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| pubmed:year |
2006
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| pubmed:articleTitle |
9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization.
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| pubmed:affiliation |
Institute of Pharmaceutical and Medicinal Chemistry, Westphalian Wilhelms-University, Hittorfstrasse 58-62, D-48149 Münster, Germany.
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| pubmed:publicationType |
Journal Article
|