Carborane-Based Carbonic Anhydrase Inhibitors

被引:84
作者
Brynda, Jiri [1 ,2 ]
Mader, Pavel [1 ]
Sicha, Vaclav [3 ]
Fabry, Milan [1 ]
Poncova, Kristyna [2 ]
Bakardiev, Mario [3 ]
Gruener, Bohumir [3 ]
Cigler, Petr [2 ]
Rezacova, Pavlina [1 ,2 ]
机构
[1] Acad Sci Czech Republ, Inst Mol Genet, Vvi, Prague 14220 4, Czech Republic
[2] Acad Sci Czech Republ, Inst Organ Chem & Biochem, Vvi, Prague 16610 6, Czech Republic
[3] Acad Sci Czech Republ, Inst Inorgan Chem, Vvi, Prague 25068, Czech Republic
关键词
carbonic anhydrases; carboranes; drug discovery; inhibitors; structure elucidation; DRUG DISCOVERY; BORON; PHARMACOPHORES;
D O I
10.1002/anie.201307583
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
CA inhibitors: Human carbonic anhydrases (CAs) are diagnostic and therapeutic targets. Various carborane cages are shown to act as active-site-directed inhibitors, and substitution with a sulfamide group and other substituents leads to compounds with high selectivity towards the cancer-specific isozyme IX. Crystal structures of the carboranes in the active site provide information that can be applied to the structure-based design of specific inhibitors. Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
引用
收藏
页码:13760 / 13763
页数:4
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