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Discovery of Strecker-type α-aminonitriles as a new class of human carbonic anhydrase inhibitors using differential scanning fluorimetry.
Krasavin, Mikhail; Stavniichuk, Roman; Zozulya, Sergey; Borysko, Petro; Vullo, Daniela; Supuran, Claudiu T.
Affiliation
  • Krasavin M; a Institute of Chemistry and Translational Biomedicine, Saint Petersburg State University , Peterhof , Russian Federation .
  • Stavniichuk R; b Enamine Ltd , Kyiv , Ukraine .
  • Zozulya S; b Enamine Ltd , Kyiv , Ukraine .
  • Borysko P; c Taras Shevchenko National University , Kyiv , Ukraine , and.
  • Vullo D; b Enamine Ltd , Kyiv , Ukraine .
  • Supuran CT; d Neurofarba Department, Universita degli Studi di Firenze , Florence , Italy.
J Enzyme Inhib Med Chem ; 31(6): 1707-11, 2016 Dec.
Article in En | MEDLINE | ID: mdl-26983069
ABSTRACT
A new type of carbonic anhydrase inhibitors was identified via differential scanning fluorimetry (DSF) screening. The compounds displayed interesting inhibition profile against human carbonic anhydrase isoforms I, II, IX and XII with an obvious selectivity displayed by one compound toward carbonic anhydrase (CA) IX, an established anti-cancer target. A hypothetical mechanism of inhibitory action by the Strecker-type α-aminonitriles has been proposed.
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Full text: 1 Database: MEDLINE Main subject: Carbonic Anhydrase Inhibitors / Fluorometry / Nitriles Language: En Year: 2016 Type: Article

Full text: 1 Database: MEDLINE Main subject: Carbonic Anhydrase Inhibitors / Fluorometry / Nitriles Language: En Year: 2016 Type: Article