Nucleoside analogues as highly potent and selective inhibitors of herpes simplex virus thymidine kinase

J A Martin; R W Lambert; J H Merrett; K E Parkes; G J Thomas; S J Baker; D J Bushnell; J E Cansfield; S J Dunsdon; A C Freeman; R A Hopkins; I R Johns; E Keech; H Simmonite; A Walmsley; P Wong Kai-In; M Holland

doi:10.1016/s0960-894x(01)00256-6

Nucleoside analogues as highly potent and selective inhibitors of herpes simplex virus thymidine kinase

Bioorg Med Chem Lett. 2001 Jul 9;11(13):1655-8. doi: 10.1016/s0960-894x(01)00256-6.

Authors

J A Martin¹, R W Lambert, J H Merrett, K E Parkes, G J Thomas, S J Baker, D J Bushnell, J E Cansfield, S J Dunsdon, A C Freeman, R A Hopkins, I R Johns, E Keech, H Simmonite, A Walmsley, P Wong Kai-In, M Holland

Affiliation

¹ Department of Medicinal Chemistry, Roche Discovery Welwyn, Broadwater Road, Welwyn Garden City, AL7 3AY, Herts, UK. joseph.martin@roche.com

PMID: 11425530
DOI: 10.1016/s0960-894x(01)00256-6

Abstract

A series of carboxamide derivatives of 5'-amino-2',5'-dideoxy-5-ethyluridine has been prepared as inhibitors of HSV-TK (herpes simplex virus thymidine kinase). The most potent compounds were derived from xanthene, thioxanthene and dihydroanthracene carboxylic acids. The lead compounds show subnanomolar IC(50) values against HSV TKs.

MeSH terms

Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Simplexvirus / enzymology*
Thymidine Kinase / antagonists & inhibitors*
Uridine / analogs & derivatives
Uridine / chemistry
Uridine / pharmacology*

Substances

5'-amino-2',5'-dideoxy-5-ethyluridine
Enzyme Inhibitors
Thymidine Kinase
Uridine