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有机锗倍半氧化物类化合物的合成

SYNTHESIS OF ORGANIC GERMANIUM SESQUIOXIDE

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【作者】 胡璧; 周则卫; 叶云鹏; 田原; 刘正明;

【Author】 Hu Bi (Hu B), Zhou Zewei (Zhou ZW), Ye Yunpeng (Ye YP), Tian Yuan (Tian Y) and Liu Zhengming (Liu ZM) (Institute of Radiation Medicine, Chinese Academy of Medical Sciences and Peking Union Medical College, Tianjin 300192)

【机构】 中国医学科学院、中国协和医科大学放射医学研究所!天津300192; 中国医学科学院、中国协?;

【摘要】 目的:为寻找新型低毒有效放射增敏剂,合成了3 种类型有机锗倍半氧化物。方法:取代桂皮酸或取代苯丙炔酸与三氯锗仿反应,所得加成物经水解即得锗倍半氧化物;三氯锗基丙酰氯与亮氨酸乙酯或苯丙氨酸乙酯反应,所得产物水解即得N(β倍半氧锗基丙酰) 氨基酸酯。结果:合成的8 个化合物中,7 个(2 ~8) 为新化合物,羧基β( 取代苯基)乙烯基锗倍半氧化物为新类型化合物。结论:离体和整体实验结果表明,化合物4 有较显著的放射增敏作用,为新型低毒有效放射增敏剂。

【Abstract】 AIM: To search for more effective and less toxic new type radiosensitizer, three types of organic germanium sesquioxide were synthesized. METHODS: 1. Substituted cinnamic acid or substituted phenyl propynoic acid reacted with trichlorogermane to afford the addition products which were hydrolyzed to the corresponding germanium sesquioxide. 2. β trichlorogermyl propionyl chloride reacted with ethyl ester of leucine or phenyl alanine to give the products which were hydrolyzed to the corresponding germanium sesquioxide. RESULTS: Eight germanium sesquioxides were synthesized and seven of them are new compounds (2~8). The type of carboxy β (substituted phenyl) vinyl germanium is reported for the first time. The structures of the compounds have been elucidated by UV, IR, 1HNMR and elemental analysis. CONCLUSION: The synthetic compounds were tested for radiosensitizing activity, compound 4 exhibited significant radiosensitizing effect both in vitro and in vivo . Compound 4 showed great potential as a new type radiosensitizer with more effective action and lower toxicity.

【关键词】 锗倍半氧化物; 放射增敏剂;
【Key words】 germanium sesquioxide; radiosensitizer;
【基金】 国家自然科学基金
  • 【文献出处】 药学学报 ,ACTA PHARMACEUTICA SINICA , 编辑部邮箱 ,1999年11期
  • 【分类号】TQ460.6
  • 【被引频次】9
  • 【下载频次】125
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