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Small Molecule Alkoxy Oriented Selectiveness on Human Carbonic Anhydrase II and IX Inhibition.
Bozdag, Murat; Cravey, Lochlin; Combs, Jacob; Kota, Anusha; McKenna, Robert; Angeli, Andrea; Selleri, Silvia; Carta, Fabrizio; Supuran, Claudiu T.
Afiliación
  • Bozdag M; NEUROFARBA Department Sezione di Scienze Farmaceutiche e Nutraceutiche, University of Florence, Via Ugo Schiff 6 Sesto Fiorentino, 50019, Florence, Italy.
  • Cravey L; Department of Biochemistry and Molecular Biology College of Medicine, University of Florida, Gainesville, FL 32610, USA.
  • Combs J; Department of Biochemistry and Molecular Biology College of Medicine, University of Florida, Gainesville, FL 32610, USA.
  • Kota A; Department of Biochemistry and Molecular Biology College of Medicine, University of Florida, Gainesville, FL 32610, USA.
  • McKenna R; Department of Biochemistry and Molecular Biology College of Medicine, University of Florida, Gainesville, FL 32610, USA.
  • Angeli A; NEUROFARBA Department Sezione di Scienze Farmaceutiche e Nutraceutiche, University of Florence, Via Ugo Schiff 6 Sesto Fiorentino, 50019, Florence, Italy.
  • Selleri S; NEUROFARBA Department Sezione di Scienze Farmaceutiche e Nutraceutiche, University of Florence, Via Ugo Schiff 6 Sesto Fiorentino, 50019, Florence, Italy.
  • Carta F; NEUROFARBA Department Sezione di Scienze Farmaceutiche e Nutraceutiche, University of Florence, Via Ugo Schiff 6 Sesto Fiorentino, 50019, Florence, Italy.
  • Supuran CT; NEUROFARBA Department Sezione di Scienze Farmaceutiche e Nutraceutiche, University of Florence, Via Ugo Schiff 6 Sesto Fiorentino, 50019, Florence, Italy.
ChemMedChem ; 17(11): e202200148, 2022 06 03.
Article en En | MEDLINE | ID: mdl-35388618
We report aryl sulfonamide inhibitors of human carbonic anhydrase (hCA; EC 4.2.1.1) enzymes containing short ureido alkoxy tails. The inhibition potency of such compounds was investigated in vitro on the major hCA isoforms (i.e. I, II, IX, and XII). A selection of the most potent inhibitory derivatives against the hCA IX isoform (i.e. 5a, 5c, and 6c) was studied, and their binding modes on either hCA II and IX-mimic isoform were assessed by X-ray crystallography on the corresponding ligand/protein adducts. This study adds to the field of developing hCA inhibitors at molecular level the critical interactions governing ligand selectivity.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores de Anhidrasa Carbónica / Anhidrasa Carbónica II Límite: Humans Idioma: En Revista: ChemMedChem Asunto de la revista: FARMACOLOGIA / QUIMICA Año: 2022 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Alemania
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores de Anhidrasa Carbónica / Anhidrasa Carbónica II Límite: Humans Idioma: En Revista: ChemMedChem Asunto de la revista: FARMACOLOGIA / QUIMICA Año: 2022 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Alemania