期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 16, 期 20, 页码 9113-9120出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.09.032
关键词
carbonic anhydrase; sulfonamide; indole-5-sulfonamide; isoforms CA I-CA XV; CA XIV-selective inhibitor
资金
- 6th Framework Programme of the European Union (EUROXY and DeZnIT projects)
- TUBITAK (Ankara, Turkey) [2219/2008]
A series of 2-(hydrazinocarbonyl)-3-substitutedphenyl-1H-indole-5-sulfonamides possessing various 2-, 3- or 4- substituted phenyl groups with methyl-, halogeno- and methoxy- functionalities, as well as the perfluorophenyl moiety have been synthesized and evaluated as inhibitors of 13 catalytically active, mammalian carbonic anhydrase (CA, EC 4.2.1.1) isoforms, that is, CA I-CA XV (of human (h) or murine (m) origin). The new compounds were ineffective inhibitors of isozymes hCA III, hCA IV, hCA VA, hCA VB, hCA VI and mCA XIII, moderate inhibitors of hCA I, hCA VII, hCA IX and mCA XV, and excellent, low-nanomolar inhibitors of hCA II and hCA XIV. The substitution pattern of the aromatic group in the 3- position of the indole ring influenced biological activity and isozyme inhibition profiles in this series of sulfonamides. Some of the best and most selective hCA XIV and mCA XV inhibitors ever reported have been identified in this study. (C) 2008 Elsevier Ltd. All rights reserved.
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