3′-[4-Aryl-(1, 2, 3-triazol-1-yl)]-3′-deoxythymidine analogues as potent and selective inhibitors of human mitochondrial thymidine kinase

…, N Solaroli, A Karlsson, J Balzarini…

文献索引：Hernandez, Ana-Isabel; Familiar, Olga; Negri, Ana; Rodriguez-Barrios, Fatima; Gago, Federico; Karlsson, Anna; Camarasa, Maria-Jose; Balzarini, Jan; Perez-Perez, Maria-Jesus Journal of Medicinal Chemistry, 2006 , vol. 49, # 26 p. 7766 - 7773

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被引用次数: 24

摘要

In an effort to increase the potency and selectivity of earlier identified substrate-based inhibitors of mitochondrial thymidine kinase 2 (TK-2), we now describe the synthesis of new thymidine analogues containing a 4-or 5-substituted 1, 2, 3-triazol-1-yl substituent at the 3′- position of the 2′-deoxyribofuranosyl ring. These analogues were prepared by Cu-and Ru- catalyzed cycloadditions of 3′-azido-3′-deoxythymidine and the appropriate alkynes, ...