Carborane-Based Carbonic Anhydrase Inhibitors

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 isoz...

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Veröffentlicht in:Angewandte Chemie International Edition 2013-12, Vol.52 (51), p.13760-13763
Hauptverfasser: Brynda, Jiří, Mader, Pavel, Šícha, Václav, Fábry, Milan, Poncová, Kristýna, Bakardiev, Mario, Grüner, Bohumír, Cígler, Petr, Řezáčová, Pavlína
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Sprache:eng
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Zusammenfassung: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.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.201307583