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Flow synthesis and biological activity of aryl sulfonamides as selective carbonic anhydrase IX and XII inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2014 Aug 01; Vol. 24 (15), pp. 3422-5. Date of Electronic Publication: 2014 Jun 04. - Publication Year :
- 2014
-
Abstract
- A series of secondary and tertiary aryl sulfonamides were synthesized under flow conditions and evaluated for their ability to selectively inhibit tumor-associated carbonic anhydrase isoforms IX and XII. The tested compounds revealed to be highly potent CA IX inhibitors in nanomolar range, and to inhibit CA XII activity with different ranks of potencies. Remarkably, 4-methyl-N-phenyl-benzenesulfonamide was a selective nanomolar CA IX inhibitor with an IC50 of 90 nM.<br /> (Copyright © 2014 Elsevier Ltd. All rights reserved.)
- Subjects :
- Carbonic Anhydrase IX
Carbonic Anhydrase Inhibitors chemical synthesis
Carbonic Anhydrase Inhibitors chemistry
Dose-Response Relationship, Drug
Humans
Models, Molecular
Molecular Structure
Structure-Activity Relationship
Sulfonamides chemical synthesis
Sulfonamides chemistry
Antigens, Neoplasm metabolism
Carbonic Anhydrase Inhibitors pharmacology
Carbonic Anhydrases metabolism
Sulfonamides pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 24
- Issue :
- 15
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 24948563
- Full Text :
- https://doi.org/10.1016/j.bmcl.2014.05.086