Published in
Wiley, Angewandte Chemie International Edition, 51(52), p. 13760-13763, 2013
Wiley, Angewandte Chemie, 51(125), p. 14005-14008, 2013
Links
Tools
Carborane-Based Carbonic Anhydrase Inhibitors
,
Václav Šícha,
Milan Fábry,
Kristýna Poncová,
Mario Bakardiev,
Bohumír Grüner,
Petr Cígler,
Pavlína Řezáčová
Full text: Download
Abstract
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.