化学学报 ›› 1962, Vol. 28 ›› Issue (4): 212-230. 上一篇    下一篇

论文

肿瘤的化学治疗 ⅩⅣ. 与放线菌素有关的化合物——2-氨基-吩噁嗪酮-(3)-衍生物的合成

趙樹緯, 高怡生   

  1. 中国科学院药物研究所
  • 投稿日期:1961-12-28 发布日期:2013-06-03

TUMOUR CHEMOTHERAPY ⅪⅤ. SYNTHESIS OF COMPOUNDS RELATED TO ACTINOMYCINS—DERIVATIVES OF 2-AMINO-PHENOXAZONE-(3)

CHAO SHU-WEI, KAO YEE-SHENG   

  1. Institute of Materia Medica, Academia Sinica
  • Received:1961-12-28 Published:2013-06-03

1.本文叙述三系列共十九种与放线菌素有关的类似物——吩噁嗪酮-(3)衍生物的合成.2.2-硝基3-甲氧基-4-取代基-苯甲酸(Ⅳa—c, R=OCH3、OC2H5及CH3)与强碱水溶液共热时, 可选择水解邻位于硝基的醚键, 生成相应的邻硝基酚衍生物(Va—c).3.作者等提出一将邻-氨基酚类化合物(Ⅻa、Ⅻc、Ⅻd及Ⅻi)氧化成2-氨基-吩噁酮-(3)衍生物(ⅩⅫa、ⅩⅫc、ⅩⅫd及ⅩⅫi)的新方法, 即在中性乙醇溶液中以钯-炭或Raney镍为催化剂, 用空气氧进行氧化.此法操作简便, 产量尚佳, 克服某些邻-氯基酚类化合物在磷酸缓冲液或碳酸铵稀醇溶液中溶解度小的困难.4.初步药理实验结果表明, 肉瘤180(固体型)对某些所合成的化合物敏感.结果将在他处发表.

The actinomycins, particularly actinomycin-C, -D, and -K are effective in inhibiting the growth of some experimental animal as well as human tumours in extremely small doses in comparison with other antitumour drugs so far known.In view of the fact that the chemical structures of these antitumourous antibiotics possess the same chromophore grouping but differ in the polypeptido-lactone-ring moiety with respect to the kinds and number of amino-acids and the sequence of their arrangement, it is suspected that the antitumour action of these compounds may arise from the chromophore grouping in common, whereas the peptido moiety functions as the carrier of the active group.