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Angew Chem Int Ed Engl
; 52(51): 13760-3, 2013 Dec 16.
Article
in English
| MEDLINE
| ID: mdl-24307504
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 isozymeâ IX. Crystal structures of the carboranes in the active site provide information that can be applied to the structure-based design of specific inhibitors.