Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 21, Pages 7413-7421Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.09.011
Keywords
Carbonic anhydrase isozymes I, II, VII, and XIII; Isothermal titration calorimetry; Thermal shift assay; ThermoFluor (R); Benzenesulfonamide; Pyrimidine
Funding
- EEA
- Norway Grants [2004-LT0019-IP-1EEE]
- Lithuanian Government
- European Community [226716]
- Research Council of Lithuania
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A series of 4-[N-(substituted 4-pyrimidinyl)amino] benzenesulfonamides were designed and synthesised. Their binding potencies as inhibitors of selected recombinant human carbonic anhydrase (hCA) isozymes I, II, VII, and XIII were measured using isothermal titration calorimetry and the thermal shift assay. To determine the structural features of inhibitor binding, the crystal structures of several compounds in complex with hCA II were determined. Several compounds exhibited selectivity towards isozymes I, II, and XIII, and some were potent inhibitors of hCA VII. (C) 2010 Elsevier Ltd. All rights reserved.
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