ISOQUINO[2,1-<i>c</i>][1,3,2] BENZODIAZAPHOSPHORINE DERIVATIVES: NEW POTENTIAL AGENTS FOR CANCER CHEMOTHERAPY
作者:E.O. John Bull、M. S. R. Naidu
DOI:10.1080/10426500008045223
日期:2000.7
relationships were indicated for antitumor activity in this screen. An aziridinyl substituted derivative, bis-(2-chloroethyl)amino substitution (3) also exhibited significant activity against the growth of P-388 lymphocytic Leukemia cells in male BDF, mice (% T/C = 147; % T/C > 125 is considered significant). The reference for activity comparison is cyclophosphamide or cytoxan i.e. [bis(2-chloroethyl)aino]-5
摘要 合成了 2-chloro-5,8,9,13b-四氢-5-methyl-6H-Isoquino[2,1-GI[1,3,2]benzodiazaphosphorine 6-oxides及其硫化物的三种衍生物。评估其抗肿瘤特性的目的。发现 21 种化合物中的 3 种在艾氏腹水癌筛查中具有显着活性(抑制肿瘤生长 > 80%)。在该筛选中显示了抗肿瘤活性的几种构效关系。氮丙啶基取代衍生物,双-(2-氯乙基)氨基取代 (3) 也表现出显着的抑制 P-388 淋巴细胞白血病细胞在雄性 BDF、小鼠中的生长的活性(% T/C = 147;% T/C > 125被认为是重要的)。活性比较的参考是环磷酰胺或环磷酰胺,即[双(2-氯乙基)氨基]-5,6-二氢-2H-1,3,