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Carbonic anhydrase inhibition with benzenesulfonamides and tetrafluorobenzenesulfonamides obtained via click chemistry

Pala, Nicolino and Micheletto, Laura and Sechi, Mario and Aggarwal, Mayank and Carta, Fabrizio and McKenna, Robert and Supuran, Claudiu T. (2013) Carbonic anhydrase inhibition with benzenesulfonamides and tetrafluorobenzenesulfonamides obtained via click chemistry. ACS Medicinal Chemistry Letters, Vol. 5 (8), p. 927-930. eISSN 1948-5875. Article.

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DOI: 10.1021/ml500196t

Abstract

A series of novel benzene- and 2,3,5,6-tetrafluorobenzenesulfonamide was synthesized by using a click chemistry approach starting from azido-substituted sulfonamides and alkynes, incorporating aryl, alkyl, cycloalkyl, and amino-/hydroxy-/halogenoalkyl moieties. The new compounds were medium potency inhibitors of the cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isoforms I and II and low nanomolar/subnanomolar inhibitors of the tumor-associated hCA IX and XII isoforms. The X-ray crystal structure of two such sulfonamides in adduct with hCA II allowed us to understand the factors governing inhibitory power.

Item Type:Article
ID Code:9919
Status:Published
Refereed:Yes
Uncontrolled Keywords:Carbonic anhydrase, click chemistry, human isoform I, human isoform II, human isoform IX, human isoform XII, benzenesulfonamide
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Chimica e Farmacia
Publisher:American Chemical Society
eISSN:1948-5875
Deposited On:25 Jun 2014 12:30

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