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Carborane‐Based Carbonic Anhydrase Inhibitors
Author(s) -
Brynda Jiří,
Mader Pavel,
Šícha Václav,
Fábry Milan,
Poncová Kristýna,
Bakardiev Mario,
Grüner Bohumír,
Cígler Petr,
Řezáčová Pavlína
Publication year - 2013
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201307583
Subject(s) - sulfamide , carbonic anhydrase , carborane , chemistry , active site , computational biology , isozyme , combinatorial chemistry , enzyme , computer science , biochemistry , stereochemistry , biology , organic chemistry
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.