【摘要】 哒嗪(5,6-diphenylpyridazin-3-one,PD)衍生物对微管体外聚合有不同程度的抑制作用,PD031至PD038对微管聚合的50％抑制浓度依次为23,10,4.5,56.48.30,>100,>100μmol/L。这些化合物对L1210白血病细胞和B16黑色素瘤细胞生长也有相应的抑制作用。进行了PD032对S-180和艾氏腹水癌的体内抗肿瘤作用的研究,100mg /kg×10(ip),治疗组小鼠生存期分别延长90％和227％,并且有3只及6只小鼠生存期超过60天。更多还原

【Abstract】 Eight synthetic PD (5,6-diphenylpyridazin-3-one) derivatives inhibited microtubule polymerization in vitro of different degrees. The concentration for 50% inhibition of PD031, PD032, PD033, PD034, PD035, PD036, PD037 and PD038 -was 23, 10, 4.5, 56, 48, 30, >100, >100μmol/L, respectively. The growth of leukemia L1210 cells and B16 melanoma cells was depressed by these compounds, among them PD032 being the most potent. The depression of these compounds on tumor growth of Sarcomal80 and Ehr-lich carcinoma in vivo was studied. At dosage of 100 mg/kg ×10 (ip), the life-span of animal treated with PD032 was increased by 90% in S-180 and 227%in Ehrlich carcinoma bearing mice, 3 (S-180) and 6 (Ehrlich) bearing mice being survived over 60 days.更多还原