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2005
Thiourea derivatives
Q 0650
Carbonic Anhydrase Inhibitors: Synthesis and Inhibition of Cytosolic/TumorCarbonic Anhydrase Isozymes I, II, and IX with Sulfonamides Incor35- 105 -Associated
porating Thioureido-Sulfanilyl Scaffolds. — A series of aromatic sulfonamides
incorporating thioureido-sulfanilyl moieties (VII) (12 examples) are synthesized and
evaluated for their interaction with the catalytic domain of human isoenzyme hCA IX
as well as the cytosolic isozymes I and II. Some of these compounds show excellent
inhibitory properties against isozymes CA I, II, and IX, as well as some specificity for
inhibiting the last isozyme over the ubiquitous cytosolic isoform CA II. —
(PUCCETTI, L.; FASOLIS, G.; CECCHI, A.; WINUM, J.-Y.; GAMBERI, A.;
MONTERO, J.-L.; SCOZZAFAVA, A.; SUPURAN*, C. T.; Bioorg. Med. Chem. Lett.
15 (2005) 9, 2359-2364; Lab. Chim. Inorg. Bioinorg., Univ. Stud. Firenze, I-50019
Sesto Fiorentino, Italy; Eng.) — R. Langenstrassen
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