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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

N1-substituted thymine derivatives as mitochondrial thymidine kinase (TK-2) inhibitors.

Novel N1-substituted thymine derivatives related to 1-[(Z)-4-(triphenylmethoxy)-2-butenyl]thymine have been synthesized and evaluated against thymidine kinase-2 (TK-2) and related nucleoside kinases [i.e., Drosophila melanogaster deoxynucleoside kinase (Dm-dNK) and herpes simplex virus type 1 thymidine kinase (HSV-1 TK)]. The thymine base has been tethered to a distal triphenylmethoxy moiety through a polymethylene chain (n = 3-8) or through a (2-ethoxy)ethyl spacer. Moreover, substitutions at position 4 of one of the phenyl rings of the triphenylmethoxy moiety have been performed. Compounds with a hexamethylene spacer (18, 26b, 31) displayed the highest inhibitory values against TK-2 (IC50 = 0.3-0.5 microM). Compound 26b competitively inhibited TK-2 with respect to thymidine and uncompetitively with respect to ATP. A rationale for the biological data was provided by docking some representative inhibitors into a homology-based model of human TK-2. Moreover, two of the most potent TK-2 inhibitors (18 and 26b) that also inhibit HSV-1 TK were able to reverse the cytostatic activity of 1-(beta-D-arabinofuranosyl)thymine (Ara-T) and ganciclovir in HSV-1 TK-expressing OST-TK-/HSV-1 TK+ cell cultures.[1]


  1. N1-substituted thymine derivatives as mitochondrial thymidine kinase (TK-2) inhibitors. Hernandez, A.I., Familiar, O., Negri, A., Rodríguez-Barrios, F., Gago, F., Karlsson, A., Camarasa, M.J., Balzarini, J., Pérez-Pérez, M.J. J. Med. Chem. (2006) [Pubmed]
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