دورية أكاديمية
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides derived from 4-isothiocyanato-benzolamide.
| العنوان: | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides derived from 4-isothiocyanato-benzolamide. |
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| المؤلفون: | Cecchi A; Università degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence), Italy., Winum JY, Innocenti A, Vullo D, Montero JL, Scozzafava A, Supuran CT |
| المصدر: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2004 Dec 06; Vol. 14 (23), pp. 5775-80. |
| نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print Cited Medium: Print ISSN: 0960-894X (Print) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Oxford : Elsevier Science Ltd Original Publication: Oxford ; New York : Pergamon Press, c1991- |
| مواضيع طبية MeSH: | Benzolamide/*chemical synthesis , Carbonic Anhydrase I/*antagonists & inhibitors , Carbonic Anhydrase II/*antagonists & inhibitors , Carbonic Anhydrase Inhibitors/*chemical synthesis , Nerve Tissue Proteins/*antagonists & inhibitors, Benzolamide/pharmacology ; Carbonic Anhydrase I/metabolism ; Carbonic Anhydrase II/metabolism ; Carbonic Anhydrase Inhibitors/pharmacology ; Carbonic Anhydrases/metabolism ; Cytosol/drug effects ; Cytosol/enzymology ; Humans ; Neoplasms/enzymology ; Nerve Tissue Proteins/metabolism ; Sulfonamides/chemical synthesis ; Sulfonamides/pharmacology |
| مستخلص: | A series of sulfonamides incorporating 4-thioureido-benzolamide moieties have been prepared from aminobenzolamide and thiophosgene followed by the reaction of the thiocyanato intermediate with aliphatic/aromatic amines or hydrazines. The new derivatives have been investigated as inhibitors of the zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1), and more precisely of the cytosolic isozymes hCA I and II, as well as the tumor-associated isozyme hCA IX (all of human origin). The new compounds showed excellent inhibitory properties against all three isozymes with inhibition constants in the range of 0.6-62 nM against hCA I, 0.5-1.7 nM against hCA II and 3.2-23 nM against hCA IX, respectively. These derivatives are interesting candidates for the development of novel therapies targeting hypoxic tumors. |
| المشرفين على المادة: | 0 (Carbonic Anhydrase Inhibitors) 0 (Nerve Tissue Proteins) 0 (Sulfonamides) EC 4.2.1.- (Carbonic Anhydrase I) EC 4.2.1.- (Carbonic Anhydrase II) EC 4.2.1.1 (Carbonic Anhydrases) FC5AAH89R5 (Benzolamide) |
| تواريخ الأحداث: | Date Created: 20041027 Date Completed: 20050322 Latest Revision: 20131121 |
| رمز التحديث: | 20231215 |
| DOI: | 10.1016/j.bmcl.2004.09.062 |
| PMID: | 15501039 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 0960-894X |
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| DOI: | 10.1016/j.bmcl.2004.09.062 |