化学学报 ›› 1962, Vol. 28 ›› Issue (5): 333-340. 上一篇    下一篇

论文

肿瘤的化学治疗——Ⅹ.氯霉素氮芥类衍生物的合成

任云峯, 赵树纬, 高怡生   

  1. 中国科学院药物研究所
  • 投稿日期:1962-04-05 发布日期:2013-06-03

TUMOUR CHEMOTHERAPY Ⅹ. NITROGEN MUSTARDS DERIVED FROM CH-LORAMPHENICOL

JEN YUN-FENG, CHOW SHU-WEI, KAO YEE-SHENG   

  1. Institute of Materia Medica, Academia Sinica, Shanghai
  • Received:1962-04-05 Published:2013-06-03

1.本文报告自对-双(2-氯乙基)氨基苯甲酸(Ⅳ)或双(2-氯乙基)氨基苯(Ⅷ)开始,分别经八步或七步反应合成1-[对-双(2-氯乙基)氦基苯基]1-2-二氯乙酰胺基-1,3-丙二醇(Ⅲa)以及1-[对-双(2-氯乙基)氨基苯基]-2-乙酰胺基-1,3-丙二醇(Ⅲb)。2.化合物Ⅲa及其中圈体X对某些动物肿瘤具显著的抑制作用。

In a previous paper,Kao and collaborators have reported the synthesis and the antitumour activity of several analogues of chloramphenicol(Ⅰ),among which 2-[p-bis(2-chloroethyl) aminobenzylidene-imino]-1-p-nitrophenyl-l,3-propanediol(Ⅱ,designated as AT-16) exhibited a pronounced inhibitory action against a variety of animalhad been and had been subjected to clinical trials.Since it has been established that the aminopropanediol moiety of chloramphenicol is necessary to the exhibition of the antibiotic action,whereas the nitro group on the phenyl ring can be changed to some other radicals without affecting the biological activity,it seems reasonable to assume that replacement of the nitro group on the ring by other groupings with potential antitumour action would be more favourable for enhancing the effectiveness in inhibiting the growth of tumours.