Abstract |
Tertiary substituted (fluorinated) benzenesulfonamides were synthesized in superacid HF/SbF5 and tested as inhibitors of human carbonic anhydrases (hCAs, EC 4.2.1.1). Strong selectivity toward tumor-associated hCA IX, without inhibiting the offtarget hCA II, was observed, pointing out to a new mechanism of action compared to classical sulfonamides.
|
Authors | Benoît Métayer, Agnès Mingot, Daniella Vullo, Claudiu T Supuran, Sébastien Thibaudeau |
Journal | Chemical communications (Cambridge, England)
(Chem Commun (Camb))
Vol. 49
Issue 54
Pg. 6015-7
(Jul 11 2013)
ISSN: 1364-548X [Electronic] England |
PMID | 23503420
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
|
Chemical References |
- Antigens, Neoplasm
- Carbonic Anhydrase Inhibitors
- Sulfonamides
- Carbonic Anhydrase II
- CA9 protein, human
- Carbonic Anhydrase IX
- Carbonic Anhydrases
|
Topics |
- Antigens, Neoplasm
(chemistry, metabolism)
- Carbonic Anhydrase II
(antagonists & inhibitors, metabolism)
- Carbonic Anhydrase IX
- Carbonic Anhydrase Inhibitors
(chemical synthesis, chemistry, metabolism)
- Carbonic Anhydrases
(chemistry, metabolism)
- Humans
- Protein Binding
- Structure-Activity Relationship
- Sulfonamides
(chemical synthesis, chemistry, metabolism)
|