First evaluation of organotellurium derivatives as carbonic anhydrase I, II, IV, VII and IX inhibitors

被引：40

作者：

Angeli, Andrea ^{[1
]}

Tanini, Damiano ^{[2
]}

Capperucci, Antonella ^{[2
]}

Supuran, Claudiu T. ^{[1
]}

机构：

[1] Dept Univ Florence, NEUROFARBA Dept, Sez Sci Farmaceut, Via Ugo Schiff 6, I-50019 Florence, Italy

[2] Dept Univ Florence, Dept Chem Ugo Schiff`, Via Lastruccia 13, I-50019 Sesto Fiorentino, Italy

来源：

BIOORGANIC CHEMISTRY | 2018年 / 76卷

关键词：

Carbonic anhydrase; Inhibitor; Metalloenzymes; Tellurium; Telluride; DRUG DISCOVERY; ISOZYME-II; PH; NANOSTRUCTURES; ANTIOXIDANT; ACTIVATORS; TELLURITE; COMPOUND; MOIETIES; AS-101;

D O I：

10.1016/j.bioorg.2017.12.010

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of tellurides was evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors against the human (h) carbonic anhydrase isoforms hCA I, II, IV, VII and IX, involved in a variety of diseases, including glaucoma, retinitis pigmentosa, epilepsy, arthritis and tumors. These compounds, which are the first tellurium-containing derivatives acting as inhibitors of carbonic anhydrase enzymes, showed effective inhibition against all isoforms investigated and some of them were selective for inhibiting the cytosolic or the membrane-bound CAs. Thus, these carbonic anhydrase inhibitors are interesting leads for the development of isoform-selective inhibitors. (C) 2017 Elsevier Inc. All rights reserved.

引用

收藏

页码：268 / 272

页数：5

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