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4-Functionalized 1,3-diarylpyrazoles bearing benzenesulfonamide moiety as selective potent inhibitors of the tumor associated carbonic anhydrase isoforms IX and XII.
Khloya, Poonam; Celik, Gulsah; Vullo, Daniela; Supuran, Claudiu T; Sharma, Pawan K.
Afiliación
  • Khloya P; Department of Chemistry, Kurukshetra University, Kurukshetra 136119, India.
  • Celik G; Chemistry Department, Balikesir University, 10145 Balikesir, Turkey.
  • SitaRam; Department of Chemistry, Kurukshetra University, Kurukshetra 136119, India.
  • Vullo D; Università degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy.
  • Supuran CT; Università degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy; Università degli Studi di Firenze, Neurofarba Dept., Section of Pharmaceutical and Nutraceutical Sciences, Via U. Schiff 6, 50019 Sesto
  • Sharma PK; Department of Chemistry, Kurukshetra University, Kurukshetra 136119, India. Electronic address: pksharma@kuk.ac.in.
Eur J Med Chem ; 76: 284-90, 2014 Apr 09.
Article en En | MEDLINE | ID: mdl-24589484
A library of 4-functionalized 1,3-diarylpyrazoles (3a-3h, 5a-5g and 6a-6g) was designed, synthesized and evaluated against four human carbonic anhydrase (CA, EC 4.2.1.1) isozymes representing two cytosolic isozymes hCA I and hCA II, and two transmembrane tumor associated ones, hCA IX and hCA XII. All the twenty two tested compounds exhibited excellent CA activity profile against the four CA isozymes when compared to the reference drug acetazolamide. Six of the tested compounds (3a-3b, 3f, 3h, 6a and 6b) displayed low nanomolar affinity (Ki < 5 nM) for hCA IX whereas seven compounds (3a-3b, 3d-3f, 3h and 6f) displayed Ki < 10 nM against hCA XII. In addition, they acted as selective CA inhibitors of isoforms IX and XII over the physiological isoforms I and II.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Sulfonamidas / Inhibidores de Anhidrasa Carbónica / Anhidrasas Carbónicas / Antígenos de Neoplasias Tipo de estudio: Risk_factors_studies Límite: Humans Idioma: En Revista: Eur J Med Chem Año: 2014 Tipo del documento: Article País de afiliación: India Pais de publicación: Francia
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Sulfonamidas / Inhibidores de Anhidrasa Carbónica / Anhidrasas Carbónicas / Antígenos de Neoplasias Tipo de estudio: Risk_factors_studies Límite: Humans Idioma: En Revista: Eur J Med Chem Año: 2014 Tipo del documento: Article País de afiliación: India Pais de publicación: Francia