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Novel 2-substituted-benzimidazole-6-sulfonamides as carbonic anhydrase inhibitors: synthesis, biological evaluation against isoforms I, II, IX and XII and molecular docking studies

Authors :
Ciro Milite
Giorgio Amendola
Alessio Nocentini
Silvia Bua
Alessandra Cipriano
Elisabetta Barresi
Alessandra Feoli
Ettore Novellino
Federico Da Settimo
Claudiu T. Supuran
Sabrina Castellano
Sandro Cosconati
Sabrina Taliani
Source :
Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 34, Iss 1, Pp 1697-1710 (2019)
Publication Year :
2019
Publisher :
Taylor & Francis Group, 2019.

Abstract

Inhibition of Carbonic Anhydrases (CAs) has been clinically exploited for many decades for a variety of therapeutic applications. Within a research project aimed at developing novel classes of CA inhibitors (CAIs) with a proper selectivity for certain isoforms, a series of derivatives featuring the 2-substituted-benzimidazole-6-sulfonamide scaffold, conceived as frozen analogs of Schiff bases and secondary amines previously reported in the literature as CAIs, were investigated. Enzyme inhibition assays on physiologically relevant human CA I, II, IX and XII isoforms revealed a number of potent CAIs, showing promising selectivity profiles towards the transmembrane tumor-associated CA IX and XII enzymes. Computational studies were attained to clarify the structural determinants behind the activities and selectivity profiles of the novel inhibitors.

Details

Language :
English
ISSN :
14756366 and 14756374
Volume :
34
Issue :
1
Database :
Directory of Open Access Journals
Journal :
Journal of Enzyme Inhibition and Medicinal Chemistry
Publication Type :
Academic Journal
Accession number :
edsdoj.58d8627f9d1b40a0bf23a6ac5f027834
Document Type :
article
Full Text :
https://doi.org/10.1080/14756366.2019.1666836