β－锗代－α－氨基酸衍生物研究Ⅱ．β－锗代溶肉瘤素倍半氧化物的合成及活性测定  

STUDIES ON THE β-GERMANYL-α-AMINOACID DERIVATIVES,ⅡTHE SYNTHESIS AND ANTITUMOR ACTIVITY OF β-GERMANYL SARCOLYSINE SESQUIOXIDE

作　　者：姜凤超[1] 陈春泉[1] 

机构地区：[1]同济医科大学药学院

出　　处：《中国药物化学杂志》1994年第1期1-3,共3页Chinese Journal of Medicinal Chemistry

摘　　要：本文以苯胺为原料合成了１－｛对－［双－（β－氯乙基）氨基］－苯基｝－２－氨基－２－羧基乙基锗倍半氧化物（Ⅰ），测定了（Ⅰ）的ＬＤ５０及抑制小鼠Ｓ－１８０的活性。结果表明当腹腔注射（ｉｐ．）给药时，（Ⅰ）对小鼠Ｓ－１８０生长的抑制率为７８％，优于Ｇｅ－１３２和溶肉瘤素，且其ＬＤ５０在腹腔注射时为１７６５ｍｇ／ｋｇ，毒性远小于溶肉瘤素。p- [bis- ( β-chloroethyl)] phenyl]- 2-amino-2-carboxyethyl germanium sesquioxide was prepared from the reaction of HGeCl3 with α-amino-cinnamic acid. The composition of the above compound was studied by using IR .elementary analysis and so on. Pharmacological experimental results showed that for compound I.the ip. LD50 for mice was found to be 1765mg/kg,and a maximum inhibition of 78% of the growth of S-180 was obtained from the ip. ,whereas an inhibition of 65% was achieved at 5-Fu under the same experimental condition.

关 键 词：溶肉瘤素 合成 锗 氨基酸衍生物 

分 类 号：TQ462.5[化学工程—制药化工]