Acta Chimica Sinica ›› 1975, Vol. 33 ›› Issue (1): 71-74. Previous Articles     Next Articles

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

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.