Source:http://linkedlifedata.com/resource/pubmed/id/18513974
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
12
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pubmed:dateCreated |
2008-6-13
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pubmed:abstractText |
Cell cycle arrest of malignant cells is an important option for cancer treatment. In this study, we modified the structure of antimitotic 2-phenylindole-3-carbaldehydes by condensation with hydrazides of various benzoic and pyridine carboxylic acids. The resulting hydrazones inhibited the growth of MDA-MB 231 and MCF-7 breast cancer cells with IC(50) values of 20-30 nM for the most potent derivatives. These 2-phenylindole derivatives also exerted an inhibitory effect on the growth of both proliferating and resting U-373 MG glioblastoma cells. Though the hydrazones exhibited similar structure-activity relationships as the aldehydes, they did not inhibit tubulin polymerization as the aldehydes but were capable of blocking the cell cycle in G(2)/M phase. The cell cycle arrest was accompanied by apoptosis as demonstrated by the activation of caspase-3. Since these 2-phenylindole-based hydrazones display no structural similarity with other antitumor drugs they are interesting candidates for further development.
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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/Antimitotic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Benzoic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Caspase 3,
http://linkedlifedata.com/resource/pubmed/chemical/Hydrazones,
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridines
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
1464-3391
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
16
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6436-47
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pubmed:meshHeading |
pubmed-meshheading:18513974-Antimitotic Agents,
pubmed-meshheading:18513974-Benzoic Acids,
pubmed-meshheading:18513974-Caspase 3,
pubmed-meshheading:18513974-Cell Cycle,
pubmed-meshheading:18513974-Cell Line, Tumor,
pubmed-meshheading:18513974-Cell Proliferation,
pubmed-meshheading:18513974-Humans,
pubmed-meshheading:18513974-Hydrazones,
pubmed-meshheading:18513974-Indoles,
pubmed-meshheading:18513974-Pyridines
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pubmed:year |
2008
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pubmed:articleTitle |
Aroyl hydrazones of 2-phenylindole-3-carbaldehydes as novel antimitotic agents.
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pubmed:affiliation |
Institut für Pharmazie, Universität Regensburg, D-93040 Regensburg, Germany.
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pubmed:publicationType |
Journal Article
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