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ID: ALA1268947
Journal: Bioorg Med Chem
Title: 4-[N-(substituted 4-pyrimidinyl)amino]benzenesulfonamides as inhibitors of carbonic anhydrase isozymes I, II, VII, and XIII.
Authors: Sūdžius J, Baranauskienė L, Golovenko D, Matulienė J, Michailovienė V, Torresan J, Jachno J, Sukackaitė R, Manakova E, Gražulis S, Tumkevičius S, Matulis D.
Abstract: 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.
CiteXplore: 20889345