1. Flow synthesis and biological activity of aryl sulfonamides as selective carbonic anhydrase IX and XII inhibitors.
- Author
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Rosatelli E, Carotti A, Ceruso M, Supuran CT, and Gioiello A
- 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
- 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., (Copyright © 2014 Elsevier Ltd. All rights reserved.)
- Published
- 2014
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