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.

Design, synthesis and enzymatic activity of highly selective human mitochondrial thymidine kinase inhibitors

MANFREDINI, Stefano;BARALDI, Pier Giovanni;VERTUANI, Silvia;
2001

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.
2001
Manfredini, Stefano; Baraldi, Pier Giovanni; Durini, E.; Porcu, L.; Angusti, A.; Vertuani, Silvia; Solaroli, N.; DE CLERCQ, E.; Karlsson, A.; Balzarini, J.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/1197509
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