351523-06-3Relevant academic research and scientific papers
NUCLEOSIDE BASED PROLIFERATION IMAGING MARKERS
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Page/Page column 39-40, (2008/12/08)
Disclosed herein are novel radiolabeled nucleosides and methods for detecting cellular proliferation in a mammal, the method comprising administrating an effective amount of a radiolabeled nucleoside; the method comprising: a) administering to the mammal a diagnostically effective amount of the nucleoside to the mammal; b) allowing the nucleoside to distribute into the effective tissue; and c) imaging the tissue, wherein an increase in binding of the compound to tissue compared to a normal control level of binding indicates that the mammal is suffering from a disease involving cellular proliferation.
Synthesis and evaluation of thymidine-5′-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase
Vanheusden, Veerle,Munier-Lehmann, Helene,Pochet, Sylvie,Herdewijn, Piet,Van Calenbergh, Serge
, p. 2695 - 2698 (2007/10/03)
A number of 2′- and 3′-modified thymidine 5′-O-monophosphate analogues were synthesized as potential leads for new anti-mycobacterial drugs. Evaluation of their affinity for Mycobacterium tuberculosis thymidine monophosphate kinase showed that a 2′-halogeno substituent and a 3′-azido function are the most favorable leads for further development of potent inhibitors of this enzyme.
Design, synthesis and enzymatic activity of highly selective human mitochondrial thymidine kinase inhibitors
Manfredini, Stefano,Baraldi, Pier G.,Durini, Elisa,Porcu, Luca,Angusti, Angela,Vertuani, Silvia,Solaroli, Nicola,De Clercq, Erik,Karlsson, Anna,Balzarini, Jan
, p. 1329 - 1332 (2007/10/03)
Highly selective arabinofuranosyl nucleosides, which inhibit the mitochondrial thymidine kinase (TK-2) without affecting the closely related herpes simplex virus type 1 thymidine kinase (HSV-1 TK), varicella-zoster virus thymidine kinase (VZV-TK), cytosolic thymidine kinase (TK-1) or the multifunctional Drosophila melanogaster deoxyribonucleoside kinase (Dm-dNK), have been obtained. SAR studies indicate a close relation between the length of the substituent at the 2′ position of the arabinofuranosyl moiety and the inhibitory activity.
