Multimeric xanthates as carbonic anhydrase inhibitors

  • Marta Abellán-Flos (Contributeur)
  • Muhammet Tanç (Créateur)
  • Claudiu T. Supuran (Créateur)
  • Stephane VINCENT (Contributeur)

Ensemble de données

Description

The field of multivalent inhibition of enzymes is growing exponentially from the first reported multivalent effect on a glycosidase enzyme. However, the investigations have generally remained restricted to carbohydrate-processing enzymes. Carbonic anhydrases are ubiquitous metallo-enzymes involved in many key biological processes, that catalyze the reversible hydration/dehydration of . This study reports the first synthesis of multimeric xanthates addressing the selectivity and potency of CA multivalent inhibition. Six multivalent compounds containing three, four, and six xanthate moieties were prepared and assayed against four relevant CA isoforms together with their monovalent analogues. Some of the multimers were stronger inhibitors than the monomeric species. For hCA I, the two best molecules 18 and 20 showed an improvement of the ligand affinity of 4.8 and 2.3 per xanthate units (valence-corrected values), respectively, which corresponds to a clear multivalent effect. Moreover, the biochemical assays demonstrated that the multimeric presentation of xanthates, also affected the selectivity of the relative inhibition among the four CAs assayed.
Date mise à disposition1 nov. 2016
EditeurUniversity of Namur

Contient cette citation

Abellán-Flos, M. (Contributeur), Tanç, M. (Créateur), Supuran, C. T. (Créateur), Vincent, S. P. (Contributeur) (1 nov. 2016). Multimeric xanthates as carbonic anhydrase inhibitors. University of Namur. 10.6084/m9.figshare.3896154.v1