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ID: ALA1833965

Journal: Bioorg Med Chem Lett

Title: A new N-methyl thymine derivative comprising a dihydroxyisobutenyl unit as ligand for thymidine kinase of herpes simplex virus type 1 (HSV-1 TK).

Authors: Krištafor S, Novaković I, Gazivoda Kraljević T, Kraljević Pavelić S, Lučin P, Westermaier Y, Pernot L, Scapozza L, Ametamey SM, Raić-Malić S.

Abstract: Molecular modeling and phosphorylation assay in vitro were employed to select a novel unsaturated 1,3-dihydroxyisobutenyl thymine derivative 6 as ligand for HSV-1 TK which may be of interest as lead for the development of an positron emission tomography (PET) imaging agent. Compound 6 was successfully prepared using modified approaches. A significant improvement over the syntheses involving pathways A and B (1% and 3% overall yield, respectively), was observed using synthetic route C (14% overall yield).

CiteXplore: 21911293

DOI: 10.1016/j.bmcl.2011.07.115