4.5 Article

New 4-[(3-cyclohexyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzene-1-sulfonamides, synthesis and inhibitory activity toward carbonic anhydrase I, II, IX, XII

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 25, 期 16, 页码 3281-3284

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.05.076

关键词

Carbonic anhydrase; Sulfonamide; Tumor-associated isoform; Selective inhibitor

资金

  1. Regione Autonoma della Sardegna (RAS) [LR 7/2007 CRP-24915]

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A series of 4-[(3-cyclohexyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzene-1-sulfonamides was synthesised and the activity of the new compounds as inhibitors of hCA I, II, IX, and XII was evaluated. These new derivatives exhibited some peculiarities with respect to previously reported sulfonamide based inhibitors of CA. We observed that the nature of the substituents in the position 3 and 4 of the dihydro- thiazole ring was relevant in determining both activity and selectivity profiles. (C) 2015 Elsevier Ltd. All rights reserved.

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