| pubmed-article:14640555 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:14640555 | lifeskim:mentions | umls-concept:C2752508 | lld:lifeskim |
| pubmed-article:14640555 | lifeskim:mentions | umls-concept:C1383501 | lld:lifeskim |
| pubmed-article:14640555 | lifeskim:mentions | umls-concept:C1167322 | lld:lifeskim |
| pubmed-article:14640555 | lifeskim:mentions | umls-concept:C0007036 | lld:lifeskim |
| pubmed-article:14640555 | lifeskim:mentions | umls-concept:C0022173 | lld:lifeskim |
| pubmed-article:14640555 | lifeskim:mentions | umls-concept:C0021467 | lld:lifeskim |
| pubmed-article:14640555 | lifeskim:mentions | umls-concept:C0021469 | lld:lifeskim |
| pubmed-article:14640555 | lifeskim:mentions | umls-concept:C0144010 | lld:lifeskim |
| pubmed-article:14640555 | pubmed:issue | 25 | lld:pubmed |
| pubmed-article:14640555 | pubmed:dateCreated | 2003-12-3 | lld:pubmed |
| pubmed-article:14640555 | pubmed:abstractText | A series of aliphatic sulfamates and related derivatives incorporating cyclic/polycyclic (steroidal) moieties in their molecules has been synthesized and assayed as inhibitors of the zinc enzyme carbonic anhydrase (CA) and, more precisely, of the cytosolic isozymes CA I and II and the transmembrane, tumor-associated isozyme CA IX. The most potent CA I inhibitor was n-tetradecyl sulfamate and some (substituted)benzyl/phenethyl sulfamates (inhibition constants in the low micromolar range). Against CA II, low nanomolar inhibitors (0.7-3.4 nM) were n-decyl sulfamate and the (substituted)benzyl/phenethyl derivatives mentioned above. Effective CA II inhibition was also observed for the hydroxy/keto derivatives of dehydroepiandrosterone sulfamate. Efficient CA IX inhibitory properties, with inhibition constants in the range of 9-23 nM, were observed for the aliphatic sulfamates C(10)-C(16) (with the most potent inhibitor being the n-dodecyl derivative) and the (substituted)benzyl/phenethyl sulfamates. The inhibition profile of the three investigated isozymes with this type of compound was rather different, allowing us to hope that the preparation of CA IX-selective inhibitors is possible (selectivity ratios toward hCA IX versus hCA II in the range of 5-63 has been observed for some of these compounds, whereas for the clinically used sulfonamides this parameter is in the range of 0.23-0.51). These data are critical for the design of novel antitumor therapies, mainly for hypoxic tumors that overexpress CA IX, which are nonresponsive to radiation or chemotherapy. | lld:pubmed |
| pubmed-article:14640555 | pubmed:language | eng | lld:pubmed |
| pubmed-article:14640555 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:14640555 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:14640555 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:14640555 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:14640555 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:14640555 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:14640555 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:14640555 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:14640555 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:14640555 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:14640555 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:14640555 | pubmed:month | Dec | lld:pubmed |
| pubmed-article:14640555 | pubmed:issn | 0022-2623 | lld:pubmed |
| pubmed-article:14640555 | pubmed:author | pubmed-author:ScozzafavaAnd... | lld:pubmed |
| pubmed-article:14640555 | pubmed:author | pubmed-author:SupuranClaudi... | lld:pubmed |
| pubmed-article:14640555 | pubmed:author | pubmed-author:CasiniAngelaA | lld:pubmed |
| pubmed-article:14640555 | pubmed:author | pubmed-author:VulloDanielaD | lld:pubmed |
| pubmed-article:14640555 | pubmed:author | pubmed-author:MonteroJean-L... | lld:pubmed |
| pubmed-article:14640555 | pubmed:author | pubmed-author:WinumJean-Yve... | lld:pubmed |
| pubmed-article:14640555 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:14640555 | pubmed:day | 4 | lld:pubmed |
| pubmed-article:14640555 | pubmed:volume | 46 | lld:pubmed |
| pubmed-article:14640555 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:14640555 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:14640555 | pubmed:pagination | 5471-7 | lld:pubmed |
| pubmed-article:14640555 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
| pubmed-article:14640555 | pubmed:meshHeading | pubmed-meshheading:14640555... | lld:pubmed |
| pubmed-article:14640555 | pubmed:meshHeading | pubmed-meshheading:14640555... | lld:pubmed |
| pubmed-article:14640555 | pubmed:meshHeading | pubmed-meshheading:14640555... | lld:pubmed |
| pubmed-article:14640555 | pubmed:meshHeading | pubmed-meshheading:14640555... | lld:pubmed |
| pubmed-article:14640555 | pubmed:meshHeading | pubmed-meshheading:14640555... | lld:pubmed |
| pubmed-article:14640555 | pubmed:meshHeading | pubmed-meshheading:14640555... | lld:pubmed |
| pubmed-article:14640555 | pubmed:meshHeading | pubmed-meshheading:14640555... | lld:pubmed |
| pubmed-article:14640555 | pubmed:meshHeading | pubmed-meshheading:14640555... | lld:pubmed |
| pubmed-article:14640555 | pubmed:meshHeading | pubmed-meshheading:14640555... | lld:pubmed |
| pubmed-article:14640555 | pubmed:meshHeading | pubmed-meshheading:14640555... | lld:pubmed |
| pubmed-article:14640555 | pubmed:meshHeading | pubmed-meshheading:14640555... | lld:pubmed |
| pubmed-article:14640555 | pubmed:meshHeading | pubmed-meshheading:14640555... | lld:pubmed |
| pubmed-article:14640555 | pubmed:meshHeading | pubmed-meshheading:14640555... | lld:pubmed |
| pubmed-article:14640555 | pubmed:meshHeading | pubmed-meshheading:14640555... | lld:pubmed |
| pubmed-article:14640555 | pubmed:year | 2003 | lld:pubmed |
| pubmed-article:14640555 | pubmed:articleTitle | Carbonic anhydrase inhibitors: inhibition of transmembrane, tumor-associated isozyme IX, and cytosolic isozymes I and II with aliphatic sulfamates. | lld:pubmed |
| pubmed-article:14640555 | pubmed:affiliation | Laboratoire de Chimie Biomoléculaire, UMR 5032, Ecole Nationale Supérieure de Chimie de Montpellier, Université Montpellier II, 8 rue de l'Ecole Normale, 34296 Montpellier Cedex, France. | lld:pubmed |
| pubmed-article:14640555 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:14640555 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:14640555 | lld:chembl |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:14640555 | lld:pubmed |
