翁尊尧. 肿瘤的化学治疗Ⅲ. 几种尿嘧啶和6-甲基尿嘧啶的5-取代基衍生物J. 药学学报, 1959, 7(7): 253-258.
引用本文: 翁尊尧. 肿瘤的化学治疗Ⅲ. 几种尿嘧啶和6-甲基尿嘧啶的5-取代基衍生物J. 药学学报, 1959, 7(7): 253-258.
OWEN TSUNG-YAO. TUMOR CHEMOTHERAPY,Ⅲ.SOME 5-SUBSTITUTED DERIVATIVES OF URACIL AND 6-METHYLURACILJ. Acta Pharmaceutica Sinica, 1959, 7(7): 253-258.
Citation: OWEN TSUNG-YAO. TUMOR CHEMOTHERAPY,Ⅲ.SOME 5-SUBSTITUTED DERIVATIVES OF URACIL AND 6-METHYLURACILJ. Acta Pharmaceutica Sinica, 1959, 7(7): 253-258.

肿瘤的化学治疗Ⅲ. 几种尿嘧啶和6-甲基尿嘧啶的5-取代基衍生物

TUMOR CHEMOTHERAPY,Ⅲ.SOME 5-SUBSTITUTED DERIVATIVES OF URACIL AND 6-METHYLURACIL

  • 摘要: 1.合成了四个5-对-取代基苯偶氮尿嘧啶(Ⅴ)和六个5-对-取代基苯偶氮-6-甲基尿嘧啶.上述十个化合物口服对小白鼠艾氏腹水瘤无显著抑制作用.2.又合成了四个5-取代基尿嘧啶(Ⅶ)和八个5-取代基-6-甲基尿嘧啶(Ⅷ),此十二个化合物口服或腹腔注射对肉瘤180无明显抑制作用.

     

    Abstract: Four 5-(p-substituted-phenylazo)-uracils (Ⅴ:Ⅴa,Ⅴb,Ⅴc and Ⅴd)and six 5-(p- substituted-phenylazo)-6-methyluracils (Ⅵ:Ⅵa,Ⅵb,Ⅵc,Ⅵd,Ⅵe and Ⅵf)were pre- pared as antitumor agents,However,none of them showed any significant activity against Ehrlich ascites tumour in mice. (Ⅴa)R=C1 mp.280°dec.(Ⅵa)R=G1 mp.235°dec. (Ⅴb)R=Br mp.270°dec.(Ⅵb)R=Br mp.227°dec. (Ⅴc)R=CH3 mp.264°dec.(Ⅵc)R=CH3 mp.223°dec. (Ⅴd)R=SCN mp.171°dec.(Ⅵd)R=OCH3 mp.235°dec. (Ⅵe)R=SCN mp.147°dec. (Ⅵf)R=SCH3 mp.222°dec. A of 5-substituted uracils and methyluracils (Ⅶ:Ⅶa,Ⅶb,Ⅶc,Ⅶd and Ⅷ: Ⅷa,Ⅷb,Ⅷc,Ⅷd,Ⅷe,Ⅷf,Ⅷg,Ⅷh)were also prepared.These uracils did not show any significant inhibiting action against Sarcoma 180 in mice.The phar- macological actions of the above compounds will be reported eleswhere. *(Ⅶa)R=NO2 *(Ⅷa)R=NO2 *(Ⅶb)R=NHCHO mp.312°dec.(Ⅷb)R=NHCHO mp.290°dec.*(Ⅶc)R=NHCOCH2Cl mp.274°dec.(Ⅷc)R=NHCOCH2Cl mp.252°dec. (Ⅶd)R=NHCSNH2 mp.>320°(Ⅷd)R=NHCOCHCl2 mp.280°dec. (Ⅷe)R=NHCOCH2I mp.236°dec. (Ⅷf)R=NHCOCF3 mp.282°dec. (Ⅷg)R=NHCOOC2H5 mp.265°dec. (Ⅷh)R=NHCSNH2 mp.268°dec.

     

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