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化学学报
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化学学报 ›› 1975, Vol. 33 ›› Issue (1): 71-74. 上一篇    下一篇

论文

喜树碱衍生物的合成

潘百川, 潘纯英, 杜元华, 王肇瀛, 翁尊尧   

  1. 上海药物研究所
  • 投稿日期:1974-04-07 发布日期:2013-06-03

STUDIES ON THE DERIVATIVES OF CAMPTOTHECIN

PAN PEI-CHUAN, PAN SHUN-YING, TU YUAN-HUA, WANG SHAO-YING, OWEN TSUNG-YAO   

  1. Shanghai Institute of Materia Medica
  • Received:1974-04-07 Published:2013-06-03

PDF

536

被引次数

5

本工作研究了一些喜树碱12-取代衍生物的合成,即12-硝基-(Ⅴ),12-氨基-(Ⅵ),12-羟基-(Ⅹ),12-甲氧基-(Ⅺ),12-氰基-(Ⅻ),12-羧基-(ⅩⅢ),12-甲氧羰基-(ⅩⅣ)及12-巯基一喜-树碱(ⅩⅤ)等.取代基的位子是借核磁共振光谱确定的.喜树碱(Ⅰ)在硫酸中硝化得Ⅴ,Ⅴ经催化氢化生成Ⅵ.Ⅵ重氮化后再经适当转换而得到预期的化合物(Ⅶ～ⅩⅤ).初步药理试验结果表明,Ⅷ对小鼠白血病615有明显抑制作用.Ⅹ及Ⅺ对小鼠艾氏腹水癌的抑制作用强于Ⅰ.进一步的药理试验正在进行中.

In the present investigation,the syntheses of some 12-substituted derivatives of camptotheoin, namely, 12-vitro-(Ⅴ),12-amino-(Ⅵ), 12-hydroxy-(Ⅹ),12-methoxy-(Ⅺ),12-oyano-(Ⅻ), 12-carboxy-(ⅩⅢ),12-carbomethoxy-(ⅪⅤ) and 12-mercapto-(ⅩⅤ) oamptothecin were described.The position of the substituent was determined with the aid of NMR spectroscopy. Camptothecin (Ⅰ) was nitrated in sulfuric acid to give V, of which catalytic hydrogenation led to the formation of Ⅵ.Diazotization of Ⅵ, followed by suitable transformations gave the desired compounds (ⅦⅩⅤ).Preliminary,pharmacological tests revealed that VIII showed much stronger inhibition against L-615.Ⅹ and Ⅺ exhibited stronger inhibition against Ehrlioh ascites carcinoma than Ⅰ.Further pharmacological examination is in progress.