Synthesis, 18F??Radiolabelling and Biological Evaluations of C??6 Alkylated Pyrimidine Nucleoside Analogues

…, SM Ametamey, S Batinac, E De Clercq…

Index: Raic-Malic, Silvana; Johayem, Anass; Ametamey, Simon M.; Batinac, Sanja; De Clercq, Erik; Folkers, Gerd; Scapozza, Leonardo Nucleosides, Nucleotides and Nucleic Acids, 2004 , vol. 23, # 11 p. 1707 - 1721

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Citation Number: 27

Abstract

Synthesis of pyrimidine derivatives with a side??chain attached to the C??6 of pyrimidine ring (6–14) is reported. Target compounds 8 and 12 were subjected to in vitro phosphorylation tests, determination of their binding affinities to herpes simplex virus (HSV??1) thymidine kinase (TK) and catalytic turnover constants. Fluorinated pyrimidine derivative 12 (40 µM) exhibited better binding affinity for HSV??1 TK than acyclovir (ACV, 170 µM) and ...