Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369620 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
A series of 50 sulfamates were obtained by reacting 4-aminophenol with isocyanates followed by sulfamoylation. Most of the new compounds were nanomolar inhibitors of the tumor-associated carbonic anhydrase (CA, EC 4.2.1.1) isoforms IX and XII, whereas they inhibited less cytosolic offtarget isoforms CA I and II. Some of these sulfamates showed significant antiproliferative activity in several breast cancer cell lines, such as SKBR3, MCF10A, ZR75/1, MDA-MB-361 and MCF7, constituting interesting anticancer leads.
Graphical abstractKIs against hCA IX and XII in the low nM range for the sulfamates.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jean-Yves Winum, Fabrizio Carta, Carol Ward, Peter Mullen, David Harrison, Simon P. Langdon, Alessandro Cecchi, Andrea Scozzafava, Ian Kunkler, Claudiu T. Supuran,