有机锗倍半氧化物类化合物的合成  

SYNTHESIS OF ORGANIC GERMANIUM SESQUIOXIDE

作　　者：胡璧[1] 周则卫[1] 叶云鹏[1] 田原[1] 刘正明[1] 

机构地区：[1]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

出　　处：《药学学报》1999年第11期818-821,共4页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金

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。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 合成 

分 类 号：R981.1[医药卫生—药品] TQ463[医药卫生—药学]