Source:http://linkedlifedata.com/resource/pubmed/id/20554082
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
9
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pubmed:dateCreated |
2010-8-9
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pubmed:abstractText |
A series of 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamide (2-16) have been synthesized and investigated as inhibitors of four isoforms of zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1), that is the cytosolic ubiquitous CA I and II, and cancer-associated isozymes CA IX and XII. Against the human isozymes hCA I the new compounds showed inhibition constants in the range of 1.09-12.1 microM, against hCA II in the range of 50.5-172 nM, against hCA IX in the range of 5.2-118 nM, and against hCA XII in the range of 8.7-381 nM, respectively. Compounds 2, 3, 5-9, 11, 13 and 14 showed excellent hCA IX inhibitory efficacy, with K(I)s = 5.2-11.0 nM, being much more effective as compared to the clinically used sulfonamides AAZ, MZA, EZA, DCP and IND (K(I)s = 24-50 nM). Compounds 2, 3, 5-9, 11 and 13 were also very effective hCA XII inhibitors (K(I)s = 8.7-45.2 nM) which are comparable or more effective than those clinically used EZA and DCP (K(I)s = 22 and 50 nM), respectively.
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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/Antigens, Neoplasm,
http://linkedlifedata.com/resource/pubmed/chemical/CA9 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Carbonic Anhydrase I,
http://linkedlifedata.com/resource/pubmed/chemical/Carbonic Anhydrase II,
http://linkedlifedata.com/resource/pubmed/chemical/Carbonic Anhydrase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Carbonic Anhydrases,
http://linkedlifedata.com/resource/pubmed/chemical/Isoenzymes,
http://linkedlifedata.com/resource/pubmed/chemical/Sulfonamides,
http://linkedlifedata.com/resource/pubmed/chemical/carbonic anhydrase XII
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
1768-3254
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pubmed:author | |
pubmed:copyrightInfo |
2010 Elsevier Masson SAS. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:volume |
45
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3656-61
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pubmed:meshHeading |
pubmed-meshheading:20554082-Antigens, Neoplasm,
pubmed-meshheading:20554082-Carbonic Anhydrase I,
pubmed-meshheading:20554082-Carbonic Anhydrase II,
pubmed-meshheading:20554082-Carbonic Anhydrase Inhibitors,
pubmed-meshheading:20554082-Carbonic Anhydrases,
pubmed-meshheading:20554082-Cell Membrane,
pubmed-meshheading:20554082-Cytosol,
pubmed-meshheading:20554082-Humans,
pubmed-meshheading:20554082-Isoenzymes,
pubmed-meshheading:20554082-Neoplasms,
pubmed-meshheading:20554082-Stereoisomerism,
pubmed-meshheading:20554082-Substrate Specificity,
pubmed-meshheading:20554082-Sulfonamides
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pubmed:year |
2010
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pubmed:articleTitle |
Carbonic anhydrase inhibitors. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the human cytosolic isozymes I and II and transmembrane cancer-associated isozymes IX and XII.
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pubmed:affiliation |
Department of Organic Chemistry, Medical University of Gda?sk, Al. Gen. J. Hallera 107, 80-416 Gda?sk, Poland.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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