Source:http://linkedlifedata.com/resource/pubmed/id/19894648
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
2009-11-9
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pubmed:abstractText |
A series of N-(imidazolidin-2-ylidene)hydrazones and N-(4,5-dihydro-1H-imidazol-2-yl)-N-methylhydrazones were prepared and examined for alpha 1-, alpha 2-adrenergic and imidazoline I1, I2 receptors binding affinities as well as cytotoxic activity against human tumor cell lines. Among the compounds tested, 2-naphthaldehyde N-(imidazolidin-2-ylidene)hydrazone (3e) exhibited a significant affinity for both alpha 2-adrenergic and imidazoline I1 receptors (Ki = 94.3 nM and IC50 = 51.7 nM, respectively). Moreover, pyridine-2-carboxaldehyde N-(imidazolidin-2-ylidene)hydrazone (3l) showed the highest binding affinity to alpha 1-adrenoceptors (Ki = 24.6 nM), while quinoline-2-carboxaldehyde N-(imidazolidin-2-ylidene)hydrazone (3m) displayed the highest I2 affinity with a Ki value of 26.7 nM and a high selectivity with respect to alpha 2-adrenergic and imidazoline I1 receptors (Ki = 22470.0 nM and IC50 = 6145.0 nM, respectively). None of the tested N-(4,5-dihydro-1H-imidazol-2-yl)-N-methylhydrazones 4p-u displayed cytotoxic activity.
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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/Hydrazones,
http://linkedlifedata.com/resource/pubmed/chemical/Imidazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Imidazoline Receptors,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, alpha-1,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, alpha-2,
http://linkedlifedata.com/resource/pubmed/chemical/imidazoline I1 receptors,
http://linkedlifedata.com/resource/pubmed/chemical/imidazoline receptor 2
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pubmed:status |
MEDLINE
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pubmed:issn |
0001-6837
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
66
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
523-34
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pubmed:meshHeading |
pubmed-meshheading:19894648-Cell Line, Tumor,
pubmed-meshheading:19894648-Humans,
pubmed-meshheading:19894648-Hydrazones,
pubmed-meshheading:19894648-Imidazoles,
pubmed-meshheading:19894648-Imidazoline Receptors,
pubmed-meshheading:19894648-Inhibitory Concentration 50,
pubmed-meshheading:19894648-Receptors, Adrenergic, alpha-1,
pubmed-meshheading:19894648-Receptors, Adrenergic, alpha-2,
pubmed-meshheading:19894648-Structure-Activity Relationship
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pubmed:articleTitle |
Synthesis and biological activity of some 2-imidazolinylhydrazone derivatives.
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pubmed:affiliation |
Department of Chemical Technology of Drugs, Medical University of Gda?sk, Al. Gen. J. Hallera 107, 80-416 Gda?sk, Poland. a.kornicka@amg.gda.pl
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pubmed:publicationType |
Journal Article
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