【摘要】 <正> 在肿瘤的化学治疗中,氮芥类化合物是研究得最广泛的一类,如何提高其选择性作用是一个近年来受人注意的方向。鉴于若干苯甲醛氮芥的衍生物(Ⅰ,Ⅱ)具有明显的抗肿瘤作用,作者选择四氢咪唑和六氢嘧啶作一些苯甲醛氮芥的载体,合成1,3-双苄基四氢咪唑和1,3-双苄基六氢嘧啶的氮芥衍生物(Ⅲ_a-Ⅲ_e,Ⅳ_a-Ⅳ_c)。这些化合物均具碱性,它们在弱酸性的条件下极易水解而放出相应的苯甲醛氮芥。作者希望能利用肿瘤组织的pH较正常组织低更多还原

【Abstract】 In the present communication seven 2-substituted-1, 3-bis-(benzyl)-tetrahydroimidazoles(Ⅲ_a-Ⅲ_g) and four 2-substituted-1, 3-bis-(benzyl)-hexahydropyrimidines(Ⅳ_a-Ⅳ_d) were synthesized as potential antitumour agents. These compounds were obtained by condensing N, N’-bis-(benzyl)-ethylenediamine(or trimethylenediamine) with appropriate benzaldehyde in the presence of a few drops of piperidine. Preliminary pharmacological tests showed that compounds Ⅲ_a, Ⅲ_b and Ⅲ_c exhibited moderate inhibition(about 50%) against sarcoma 180 in mice.更多还原