Carborane-based carbonic anhydrase inhibitors
Language English Country Germany Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
- Keywords
- carbonic anhydrases, carboranes, drug discovery, inhibitors, structure elucidation,
- MeSH
- Carbonic Anhydrase Inhibitors pharmacology MeSH
- Humans MeSH
- Drug Discovery MeSH
- Drug Design MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Carbonic Anhydrase Inhibitors MeSH
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.
References provided by Crossref.org
Access to cationic polyhedral carboranes via dynamic cage surgery with N-heterocyclic carbenes