Source:http://linkedlifedata.com/resource/pubmed/id/18328669
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
2009-3-2
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pubmed:abstractText |
As part of a continuing search for new potential anticancer candidates in the piperazinyl quinolone series, the cytotoxicity evaluation of new N-substituted piperazinyl quinolones was of our interest. The growth inhibitory activities of 12 new compounds, namely N-[2-(5-chlorothiophen-2-yl)-2-oxoethyl] and N-[2-(5-chlorothiophen-2-yl)-2-oxyiminoethyl] piperazinyl quinolones 1-12 were determined against six cancer cell lines using MTT colorimetric assay. Preliminary screening showed that most of the new N-[2-(5-chlorothiophen-2-yl)ethyl]piperazinyl quinolones 4-12 containing (un)substituted oxime moiety showed significant cytotoxic activity and the modification of functionality on ethyl spacer produced a relatively minor change of activity. Thus, in the piperazinyl quinolone series, cytotoxic activity can be positively modulated through the introduction of 2-(5-chlorothiophen-2-yl)ethyl residue on the piperazine ring. The results revealed that the introduction of 2-(5-chlorothiophen-2-yl)ethyl moiety on the piperazine ring of quinolone antibacterials (ciprofloxacin, norfloxacin and enoxacin) changes the biological profile of piperazinyl quinolones from antibacterials to cytotoxic agents.
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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/Anti-Bacterial Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Quinolones,
http://linkedlifedata.com/resource/pubmed/chemical/Tetrazolium Salts,
http://linkedlifedata.com/resource/pubmed/chemical/Thiazoles,
http://linkedlifedata.com/resource/pubmed/chemical/thiazolyl blue
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
1950-6007
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:volume |
63
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
216-20
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pubmed:meshHeading |
pubmed-meshheading:18328669-Anti-Bacterial Agents,
pubmed-meshheading:18328669-Antineoplastic Agents,
pubmed-meshheading:18328669-Cell Line, Tumor,
pubmed-meshheading:18328669-Colorimetry,
pubmed-meshheading:18328669-Drug Screening Assays, Antitumor,
pubmed-meshheading:18328669-Humans,
pubmed-meshheading:18328669-Inhibitory Concentration 50,
pubmed-meshheading:18328669-Quinolones,
pubmed-meshheading:18328669-Structure-Activity Relationship,
pubmed-meshheading:18328669-Tetrazolium Salts,
pubmed-meshheading:18328669-Thiazoles
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pubmed:year |
2009
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pubmed:articleTitle |
N-Substituted piperazinyl quinolones as potential cytotoxic agents: structure-activity relationships study.
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pubmed:affiliation |
Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran 14174, Iran.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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