Bioorganic & Medicinal Chemistry Letters 2012-07-15

Ureido-substituted sulfamates show potent carbonic anhydrase IX inhibitory and antiproliferative activities against breast cancer cell lines.

Jean-Yves Winum, Fabrizio Carta, Carol Ward, Peter Mullen, David Harrison, Simon P Langdon, Alessandro Cecchi, Andrea Scozzafava, Ian Kunkler, Claudiu T Supuran, Jean-Yves Winum, Fabrizio Carta, Carol Ward, Peter Mullen, David Harrison, Simon P. Langdon, Alessandro Cecchi, Andrea Scozzafava, Ian Kunkler, Claudiu T. Supuran, Jean-Yves Winum, Fabrizio Carta, Carol Ward, Peter Mullen, David Harrison, Simon P Langdon, Alessandro Cecchi, Andrea Scozzafava, Ian Kunkler, Claudiu T Supuran

文献索引：Bioorg. Med. Chem. Lett. 22(14) , 4681-5, (2012)

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摘要

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.Copyright © 2012 Elsevier Ltd. All rights reserved.