硝基(芳亚胺基)二乙基硫代硫酸钠和硝基苯丙氮酸衍生物的合成和放射增敏作用  

SYNTHESIS AND RADIOSENSITIZING ACTIVITY OF NITROARYLIMINO-DIETHYL-SODIUM THIOSULFATE AND NITRO PHENYLALANINE DERIVATIVES

作　　者：刘汇辛 李政[2] 胡璧[1] 李政[2] 糜福顺[2] 沈瑜 

机构地区：[1]中国医学科学院放射医学研究所,天津300192 [2]中国医学科学院肿瘤研究所,北京100021

出　　处：《药学学报》1992年第8期632-637,共6页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金

摘　　要：乏氧细胞对射线所具有的较大抗性是对某些人类肿瘤进行放疗失效的主要原因。放射增敏剂的研究目的是为了提高射线在正常组织可耐受剂量下对肿瘤细胞的杀伤率,从而提高放疗效果。目前试用于临床的放射增散剂misoniizole(MISO)是一种硝基咪唑类化合物,由于其较强的神经毒性,限制了这种药物的推广和使用。为寻找新的低毒有效的放射增敏剂,我们设计并合成了一系列化合物,试验了它们对离体Hela-S_3细胞的放射增敏作用。A series of compounds was synthesized, these compounds were tested for Hela-S_3cells in vitro for radiosensitizing activity. Five of them are 2,2′- (arylimino)-diethyl-sodium thio-sulfate and two of them are phenylalanine derivatives. Most of them showed various degrees of ra-diosensitizing activity. Among them, SER of L07 was 1.89 at 3 mmol, and had low cytotoxicity toHela-S_3 cells;ID_(50) was 18.8 mmol. The relationship between radiosensitizing effects and chemicalstructure was discussed. It offers a base for further exploration of selectively hypoxic cell radiosens-itizers.

关 键 词：抗癌药 硝基苯丙氮酸 

分 类 号：R979.1[医药卫生—药品]