【摘要】 我校合成的10个取代苯甲磺酰腙衍生物,经对人白血病HL₆₀细胞杀伤能力试验表明,化合物（2）、（3）、（9）及（10）在浓度为10—50ug/ml时与癌细胞混合培养48小时,可杀死50％以上癌细胞。体内实验证明化合物（2）、（8）、（9）及（10）25mg/kg ip×7天,可使P₃₈₈白血病小鼠生命延长率分别达202.84％、63.20％、170.29％、366.17％,其中（10）还可使75％的小鼠长期存活。化合物（2）、（3）、（10）在25—50mg/kg ip×7天时,对S₁₈₀小鼠抑瘤率分别为34.41—49.62％。采用流式细胞光度术,观察化合物（10）对小鼠白血病L₁₂₁₀细胞周期动力学的影响,发现它可使癌细胞集中在G₁期,S期细胞数减少,可能为主要作用于G₁期细胞的药物。更多还原

【Abstract】 Ten new derivatives of substituted benzaldehyde arylsulfonyl-hydrazones were evaluated for antineoplastic activity against HL - 60 cells. leukemia P388 and sarcoma 180 mice. The compounds (2) ,(3),(8),(9) and (10) were recognized to possess antitu-mor activity. The compound (10) was the most potent in these compounds. It killed about 60% HL-60 cells in the culture at 10 ug/ml concentration. It was given 25mg/kg ip produced a more than 366. 17% increase life span and 75% members 60 -day survivors in mice with leukemia P388. It was also effective against sc implanted S180 mice.The effect of compound (10) on the cell cycle of mouse L1210 cells was studied by flow cytometer. The cells were blocked on the G1 phase.更多还原