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[硝基 - 芳基亚氨基 - 二乙基硫代硫酸钠和硝基苯丙氨酸衍生物的合成及放射增敏活性]

[Synthesis and radiosensitizing activity of nitro-arylimino-diethyl-sodium thiosulfate and nitro phenylalanine derivatives].

作者信息

Liu H X, Hu B, Li Z, Mi F S, Shen Y

机构信息

Institute of Radiation Medicine, Chinese Academy of Medical Sciences, Tianjin.

出版信息

Yao Xue Xue Bao. 1992;27(8):632-7.

PMID:1481683
Abstract

A series of compounds was synthesized, these compounds were tested for Hela-S3 cells in vitro for radiosensitizing activity. Five of them are 2,2'-(arylimino)-diethyl-sodium thiosulfate and two of them are phenylalanine derivatives. Most of them showed various degrees of radiosensitizing activity. Among them, SER of L07 was 1.89 at 3 mmol, and had low cytotoxicity to Hela-S3 cells, ID50 was 18.8 mmol. The relationship between radiosensitizing effects and chemical structure was discussed. It offers a base for further exploration of selectively hypoxic cell radiosensitizers.

摘要

合成了一系列化合物,对这些化合物进行了体外针对Hela-S3细胞的放射增敏活性测试。其中五种是2,2'-(芳基亚氨基)-二乙硫代硫酸钠,两种是苯丙氨酸衍生物。它们中的大多数表现出不同程度的放射增敏活性。其中,L07在3 mmol时的增敏增强率(SER)为1.89,对Hela-S3细胞的细胞毒性较低,半数抑制浓度(ID50)为18.8 mmol。讨论了放射增敏作用与化学结构之间的关系。这为进一步探索选择性低氧细胞放射增敏剂提供了依据。

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