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

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

文献索引：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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被引用次数: 27

摘要

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 ...