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化学学报
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化学学报 ›› 1982, Vol. 40 ›› Issue (11): 1070-1075. 上一篇    下一篇

研究简报

肿瘤的化学治疗——ⅩⅩⅩⅩⅣ.双(β-氯乙基)氨甲基苯丙氨酸有关化合物的研究 (四)2-双(β-氯乙基)氨甲基-5-甲氧基-苯丙氨酸双盐酸盐的合成

陈葆仁1, 洪文旺2, 任云峰2   

  1. 1. 江西医学院, 南昌;
    2. 中国科学院上海药物研究所
  • 投稿日期:1981-05-07 发布日期:2013-06-03
  • 通讯作者: 陈葆仁

TUMOUR CHEMOTHERAPY ⅩⅩⅩⅩⅣ. STUDIES ON BIS (β-CHLOROETHYL) AMINOMETHYL PHENYLALANINE 4. SYNTHESIS OF 2-BIS (β-CHLOROETHYL)-AMINOMETHYL-5-METHOXY-PHENYLALANINE

CHEN BAO-REN1, HONG WEN-WANG2, REN YUN-FENG2   

  1. 1. Jiangxi Medical College, Nanchang;
    2. Shanghai Institute of Materia Medica, Academia Sinica
  • Received:1981-05-07 Published:2013-06-03

PDF

793

被引次数

6

邻-双(β-氯乙基)氨甲基苯丙氨酸双盐酸盐(1,AT-581,邻脂苯芥)对多种动物肿瘤及临床均有效[1,2],但毒性较大.氮芥类的毒性与氮芥基中氯原子的化学活性有一定关系.一般说来,化学活性愈高,毒性愈大.

In view of the favorable antitumour aotion of bis (β-chloroethyl) aminomethyl-5-nitro-phenylalanine(2,Nitrooaphane, AT-1258) and in order to study the relationship between ohemioal structure and anti Enmour activity, the authors synthesized 2-bis (β-ohloroethyl) aminomethyl-5-methogy-phenyl alanine dihydroohlorides (4) by replacing the nitro group on the benzene ring of Nitrocaphane with the methozy group.