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200517.fm Page 223 Friday, March 18, 2005 2:52 PM
2005
Nucleic acids
U 0700
Synthesis, 18 F-Radiolabelling and Biological Evaluations of C-6 Alkylated Pyrimidine Nucleoside Analogues. — The novel pyrimidines (I), containing a substituted
17- 203 hydroxypropyl side-chain, are evaluated for their cytotoxic properties, binding affinities to herpes simplex virus (HSV-1) thymidine kinase (TK) and kinetic turnover constants. Pyrimidine derivative (Ib) displays better binding affinity for HSV-1 TK than
acyclovir and ganciclovir. Compounds (I) show no cytotoxic effects and no specific
antiviral or antitumor activities. Fluorinated pyrimidine derivative (Ib) can be phosphorylated by HSV-1 TK, thus fulfilling the requirements for application as PEt-tracer
molecule. 18F labelling of the precursor (II) is performed, although the radiochemical
yield is low. — (RAIC-MALIC*, S.; JOHAYEM, A.; AMETAMEY, S. M.; BATINAC,
S.; DE CLERCQ, E.; FOLKERS, G.; SCAPOZZA, L.; Nucleosides, Nucleotides
Nucleic Acids 23 (2004) 11, 1707-1721; Dep. Org. Chem., Fac. Chem. Eng. Technol.,
Univ. Zagreb, HR-10000 Zagreb, Croatia; Eng.) — H. Hoennerscheid
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