Hypoxia-targeting carbonic anhydrase IX inhibitors by a new series of nitroimidazole-sulfonamides/sulfamides/sulfamates

…, P Lambin, G De Simone, CT Supuran…

Index: Rami, Marouan; Dubois, Ludwig; Parvathaneni, Nanda-Kumar; Alterio, Vincenzo; Van Kuijk, Simon J. A.; Monti, Simona Maria; Lambin, Philippe; De Simone, Giuseppina; Supuran, Claudiu T.; Winum, Jean-Yves Journal of Medicinal Chemistry, 2013 , vol. 56, # 21 p. 8512 - 8520

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Citation Number: 28

Abstract

A series of nitroimidazoles incorporating sulfonamide/sulfamide/sulfamate moieties were designed and synthesized as radio/chemosensitizing agent targeting the tumor-associated carbonic anhydrase (CA) isoforms IX and XII. Most of the new compounds were nanomolar inhibitors of these isoforms. Crystallographic studies on the complex of hCA II with the lead sulfamide derivative of this series clarified the binding mode of this type of inhibitors in the ...