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Tetrahydroquinazole-based secondary sulphonamides as carbonic anhydrase inhibitors: synthesis, biological evaluation against isoforms I, II, IV, and IX, and computational studies.
Baglini, Emma; Ravichandran, Rahul; Berrino, Emanuela; Salerno, Silvia; Barresi, Elisabetta; Marini, Anna Maria; Viviano, Monica; Castellano, Sabrina; Da Settimo, Federico; Supuran, Claudiu T; Cosconati, Sandro; Taliani, Sabrina.
Affiliation
  • Baglini E; Department of Pharmacy, University of Pisa, Pisa, Italy.
  • Ravichandran R; DiSTABiF, University of Campania Luigi Vanvitelli, Caserta, Italy.
  • Berrino E; NEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze, Sesto Fiorentino, Italy.
  • Salerno S; Department of Pharmacy, University of Pisa, Pisa, Italy.
  • Barresi E; Department of Pharmacy, University of Pisa, Pisa, Italy.
  • Marini AM; Department of Pharmacy, University of Pisa, Pisa, Italy.
  • Viviano M; Department of Pharmacy, Epigenetic Med Chem Lab, University of Salerno, Fisciano, Italy.
  • Castellano S; Department of Pharmacy, Epigenetic Med Chem Lab, University of Salerno, Fisciano, Italy.
  • Da Settimo F; Department of Pharmacy, University of Pisa, Pisa, Italy.
  • Supuran CT; NEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze, Sesto Fiorentino, Italy.
  • Cosconati S; DiSTABiF, University of Campania Luigi Vanvitelli, Caserta, Italy.
  • Taliani S; Department of Pharmacy, University of Pisa, Pisa, Italy.
J Enzyme Inhib Med Chem ; 36(1): 1874-1883, 2021 Dec.
Article in En | MEDLINE | ID: mdl-34340614
ABSTRACT
A library of variously decorated N-phenyl secondary sulphonamides featuring the bicyclic tetrahydroquinazole scaffold was synthesised and biologically evaluated for their inhibitory activity against human carbonic anhydrase (hCA) I, II, IV, and IX. Of note, several compounds were identified showing submicromolar potency and excellent selectivity for the tumour-related hCA IX isoform. Structure-activity relationship data attained for various substitutions were rationalised by molecular modelling studies in terms of both inhibitory activity and selectivity.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Quinazolines / Sulfonamides / Carbonic Anhydrase Inhibitors / Computational Biology / Isoenzymes Language: En Journal: J Enzyme Inhib Med Chem Journal subject: BIOQUIMICA / QUIMICA Year: 2021 Type: Article Affiliation country: Italy

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Quinazolines / Sulfonamides / Carbonic Anhydrase Inhibitors / Computational Biology / Isoenzymes Language: En Journal: J Enzyme Inhib Med Chem Journal subject: BIOQUIMICA / QUIMICA Year: 2021 Type: Article Affiliation country: Italy