Azidothymidine “Clicked” into 1,2,3-Triazoles: First Report on Carbonic Anhydrase–Telomerase Dual-Hybrid Inhibitors
Emanuela Berrino, Andrea Angeli, Dmitry D. Zhdanov, Anna P. Kiryukhina, Andrea Milaneschi, Alessandro De Luca, Murat Bozdağ, Simone Carradori, Silvia Selleri, Gianluca Bartolucci, Thomas S. Peat, Marta Ferraroni, Claudiu T. Supuran, Fabrizio Carta
Abstract
values ranging from 5.2 to 9.1 μM). High-resolution X-ray crystallography on selected derivatives in the adduct with hCA II as a model study allowed to determine their binding modes and thus to set the structural determinants necessary for further development of compounds selectively targeting the tumoral cells.
Topics & Concepts
ChemistryCarbonic anhydraseTelomeraseDual (grammatical number)TriazoleCarbonic anhydrase IICombinatorial chemistryEnzymeBiochemistryStereochemistryPharmacologyOrganic chemistryGeneArtLiteratureMedicineClick Chemistry and ApplicationsSynthesis and Catalytic ReactionsEnzyme function and inhibition