157024-75-4Relevant articles and documents
SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY OF 2'-O-ALLYL-1-beta-D-ARABINOFURANOSYL-URACIL, -CYTOSINE AND -ADENINE
Manfredini, Stefano,Baraldi, Pier Giovanni,Bazzanini, Rita,Simoni, Daniele,Balzarini, Jan,Clercq, Erik De
, p. 473 - 478 (1997)
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3-methyl uridine and 4-methyl cytidine nucleoside compound, synthetic method and its pharmaceutical use
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Paragraph 0021; 0036, (2016/10/08)
The invention discloses a 3-methyluridine and 4-methylcytidine nucleosides compound and a synthesis method and pharmaceutical application thereof, belonging to the field of medicinal chemistry. The compound has a structural formula as shown in the specification. The compound has the effects of simultaneously modifying sugar rings and basic groups, increasing the activity of the compound and reducing the toxicity, provides a good application prospect for development of like medicines and can be applied to preparation of anti-HBV (Hepatitis B virus) medicines. The synthesis method is simple and feasible and provides conditions for mass synthesis of the compound.
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.