期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 18, 页码 5086-5090出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.07.023
关键词
carbonic anhydrase; isoforms; tumor-associated isozyme; sulfamide; sugar
A series of glycosylated sulfarnides possessing a diverse substitution pattern, with benzylated, peracetylated, and unsaturated six- and five-membered ring sugar moieties attached to the NHSO2NH2 zinc binding group is reported. These derivatives were tested for the inhibition of five human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms, hCA I, II, IV, IX, and XII. Against hCA I the sulfamides behaved as weak inhibitors, whereas they showed low nanomolar activity against hCA II, IX, and XII, being slightly less effective as hCA IV inhibitors. One compound showed selectivity for inhibiting the tumor-associated isoforms hCA IX and XII over the ubiquitous cytosolic hCA II. The sulfamide zinc binding group may thus indeed lead to very effective glycosylated inhibitors targeting several physiologically relevant isozymes. (c) 2007 Elsevier Ltd. All rights reserved.
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