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ChemInform Abstract: Design, Synthesis and Enzymatic Activity of Highly Selective Human Mitochondrial Thymidine Kinase Inhibitors

Authors :
Nicola Solaroli
Pier Giovanni Baraldi
Jan Balzarini
Angela Angusti
Anna Karlsson
Silvia Vertuani
Erik De Clercq
Elisa Durini
Stefano Manfredini
Luca Porcu
Source :
ChemInform. 32
Publication Year :
2010
Publisher :
Wiley, 2010.

Abstract

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.

Details

ISSN :
15222667 and 09317597
Volume :
32
Database :
OpenAIRE
Journal :
ChemInform
Accession number :
edsair.doi...........91bedcc752019819e313969c6397dffd
Full Text :
https://doi.org/10.1002/chin.200136225