Source:http://linkedlifedata.com/resource/pubmed/id/11858989
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
2002-2-22
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pubmed:abstractText |
The new thiosemicarbazones and thiocarbonohydrazones derived from 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane were synthesized and evaluated for their inhibitory effect on tumor cell proliferation and their antiviral and antimicrobial activity. Thiosemicarbazone inhibited tumor cell proliferation (GI50's range: 2.4-100 microM and mean GI50 43.9 microM against various human leukemic cell lines) while thiosemicarbazone and thiocarbonohydrazone 5d exhibited significant inhibition of tumor cell proliferation (GI50's range 2.3-23.6 microM and mean GI50 7.2 microM for and GI50's range 2.4-32.4 microM and mean GI50 12.8microM for ). These GI50 values are comparable to that of 2-acetylpyridine thiosemicarbazone an important lead in TSC's family. The compounds did not afford specific activity against any of the viruses tested when examined at non-toxic concentrations. A weak activity was found for thiocarbonohydrazones against Gram-(+) bacteria (MIC(50) 117.3 and 133 microM, respectively). Using a combination of molecular mechanics calculations and NOE spectroscopy it was shown that the parent compounds and have opposite configuration around C=N bond. Whether this difference in structure can be correlated with the biological activity will be investigated in future studies.
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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/Formazans,
http://linkedlifedata.com/resource/pubmed/chemical/Hydrazones,
http://linkedlifedata.com/resource/pubmed/chemical/MTT formazan,
http://linkedlifedata.com/resource/pubmed/chemical/Tetrazolium Salts,
http://linkedlifedata.com/resource/pubmed/chemical/Thiosemicarbazones
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:AndreiGracielaG,
pubmed-author:De ClercqErikE,
pubmed-author:DimasKostasK,
pubmed-author:FoscolosGeorge BGB,
pubmed-author:FytasGeorgeG,
pubmed-author:KolocourisAntoniosA,
pubmed-author:KolocourisNicolasN,
pubmed-author:PannecouqueChristopheC,
pubmed-author:SnoeckRobertR,
pubmed-author:StamatiouGeorgeG,
pubmed-author:WitvrouwMyriamM,
pubmed-author:ZoidisGrigorisG
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pubmed:issnType |
Print
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pubmed:day |
11
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pubmed:volume |
12
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
723-7
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:11858989-Bacteria,
pubmed-meshheading:11858989-Cell Division,
pubmed-meshheading:11858989-Cell Line,
pubmed-meshheading:11858989-Formazans,
pubmed-meshheading:11858989-Humans,
pubmed-meshheading:11858989-Hydrazones,
pubmed-meshheading:11858989-Microbial Sensitivity Tests,
pubmed-meshheading:11858989-Molecular Structure,
pubmed-meshheading:11858989-Structure-Activity Relationship,
pubmed-meshheading:11858989-Tetrazolium Salts,
pubmed-meshheading:11858989-Thiosemicarbazones,
pubmed-meshheading:11858989-Tumor Cells, Cultured,
pubmed-meshheading:11858989-Viruses
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pubmed:year |
2002
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pubmed:articleTitle |
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
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pubmed:affiliation |
School of Pharmacy, Department of Pharmaceutical Chemistry, University of Athens, Panepistimioupoli-Zografou, GR-15771, Athens, Greece.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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