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Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement.
Krasavin, Mikhail; Kalinin, Stanislav; Zozulya, Sergey; Griniukova, Anastasia; Borysko, Petro; Angeli, Andrea; Supuran, Claudiu T.
Afiliación
  • Krasavin M; Saint Petersburg State University, Saint Petersburg, Russian Federation.
  • Kalinin S; Saint Petersburg State University, Saint Petersburg, Russian Federation.
  • Zozulya S; Enamine Ltd, Kyiv, Ukraine.
  • Griniukova A; Taras Shevchenko National University, Kyiv, Ukraine.
  • Borysko P; Enamine Ltd, Kyiv, Ukraine.
  • Angeli A; Enamine Ltd, Kyiv, Ukraine.
  • Supuran CT; Neurofarba Department, Universita degli Studi di Firenze, Florence, Italy.
J Enzyme Inhib Med Chem ; 35(1): 165-171, 2020 Dec.
Article en En | MEDLINE | ID: mdl-31752557
ABSTRACT
Testing of an expanded, 800-compound set of analogues of the earlier described Strecker-type α-aminonitriles (selected from publicly available Enamine Ltd. Screening Collection) in thermal shift assay against bovine carbonic anhydrase (bCA) led to further validation of this new class of inhibitors and identification a new, refined chemotype represented by inhibitors with 10-improved potency. [Formula see text].
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores de Anhidrasa Carbónica / Anhidrasa Carbónica II / Nitrilos Límite: Animals / Humans Idioma: En Revista: J Enzyme Inhib Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores de Anhidrasa Carbónica / Anhidrasa Carbónica II / Nitrilos Límite: Animals / Humans Idioma: En Revista: J Enzyme Inhib Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article
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