期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 84, 期 -, 页码 240-246出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.07.014
关键词
Acesulfame derivatives; Anticancer agents; N-alkylation; O-alkylation; Selective hCA IX/hCAXII inhibitors; Sulfamate
资金
- FP7 EU project Metoxia
- FP7 EU project Dynano
Carbonic anhydrase (hCA) IX and XII isoforms are over-expressed both in primary and in metastatic cell lines of hypoxic tumors and are innovative targets for cancer diagnosis and treatment. On the basis of the importance of the pharmacophoric sulfamate moiety (bioisostere of the sulfonamide group) present in the structure of recent human CA inhibitors, we designed N-alkylated and O-allcylated derivatives of acesulfame, a cyclic tertiary sulfamate, assessing the inhibitory activity against the ubiquitous isoforms hCA I and II and the cancer-related isoforms hCA IX and XII. All derivatives were nanomolar inhibitors, with some of them possessing an outstanding selectivity towards the tumor-associated hCA IX and/or hCA XII isoforms. (c) 2014 Elsevier Masson SAS. All rights reserved.
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