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四种胸苷类似物的抗病毒作用和细胞毒性:5-乙基-、5-乙烯基-、5-丙基-和5-烯丙基-2'-脱氧尿苷

Antiviral action and cellular toxicity of four thymidine analogues: 5-ethyl-,5-vinyl-, 5-propyl-, and 5-allyl-2'- deoxyuridine.

作者信息

Cheng Y C, Domin B A, Sharma R A, Bobek M

出版信息

Antimicrob Agents Chemother. 1976 Jul;10(1):119-22. doi: 10.1128/AAC.10.1.119.

Abstract

5-Ethyl-, 5-vinyl-, 5-propyl-, and 5-allyl-2'-deoxyuridine (dUrd) had antiviral activity against herpes simplex type 1 and type 2 grown in HeLa TK(-) cells, in the order 5-vinyl-dUrd, 5-ethyl-dUrd, 5-propyl-dUrd, 5-allyl-dUrd, but they were inactive against a TK(-) mutant of herpes simplex type 1. The antiviral activity of these compounds could be partially reversed by thymidine. Except for 5-vinyl-dUrd, they were not toxic to WI-38 and HeLa TK(-) cells at a concentration of 25 muM. All four analogues inhibited the growth of herpes simplex type 1-transformed HeLa TK(-) cells at a concentration of 1 muM.

摘要

5-乙基-、5-乙烯基-、5-丙基-和5-烯丙基-2'-脱氧尿苷(dUrd)对在HeLa TK(-)细胞中生长的单纯疱疹病毒1型和2型具有抗病毒活性,其活性顺序为5-乙烯基-dUrd、5-乙基-dUrd、5-丙基-dUrd、5-烯丙基-dUrd,但它们对单纯疱疹病毒1型的TK(-)突变体无活性。这些化合物的抗病毒活性可被胸苷部分逆转。除5-乙烯基-dUrd外,它们在25 μM浓度下对WI-38和HeLa TK(-)细胞无毒。所有四种类似物在1 μM浓度下均抑制单纯疱疹病毒1型转化的HeLa TK(-)细胞的生长。

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On the mode of action of 5-vinyl-2'-deoxyuridine.关于5-乙烯基-2'-脱氧尿苷的作用模式。
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Synthesis of 5-vinyluridine and 5-vinyl-2'-deoxyuridine as new pyrimidine nucleoside analogs.
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