Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 21, Issue 13, Pages 3790-3794Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.04.041
Keywords
Dodoneine; Superacid; Metabolites; Carbonic anhydrase; Hybrid molecules
Funding
- EU
- CNRS
- University of Poitiers
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The natural product dodoneine (a dihydropyranone phenolic compound), extracted from African mistletoe Agelanthus dodoneifolius, has been investigated as inhibitor of several human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms. By using superacid chemistry, analogues of the lactone phenolic hybrid lead compound have been synthesized and tested as CA inhibitors. Small chemical modifications of the basic scaffold revealed strong changes in the selectivity profile against different CA isoforms. These new compounds selectively inhibited isoforms CA I (K(I)s in the range of 0.13-0.76 mu M), III (K(I)s in the range of 5.13-10.80 mu M), XIII (K(I)s in the range of 0.34-0.96 mu M) and XIV (K(I)s in the range of 2.44-7.24 mu M), and can be considered as new leads, probably acting as non-zinc-binders, similar to other phenols/lactones investigated earlier. (C) 2013 Elsevier Ltd. All rights reserved.
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