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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
In the chemotherapy of the tumor, nitrogen mustard compounds are the most widely studied, and how to increase their selectivity is a direction that has been paid attention in recent years. In view of the obvious anti-tumor effect of several benzofenazone derivatives (Ⅰ, Ⅱ), the authors selected tetrahydroimidazoles and hexahydropyrimidines as carriers of benzaldehyde and nitrogen mustard to synthesize 1,3-bisbenzyltetrahydroimidazole And nitrogen mustard derivatives (III_a-III_e, IV_a-IV_c) of 1,3-bis-benzylhexahydropyrimidine. These compounds are all basic, they are easily hydrolyzed in the weak acid conditions and emit the corresponding benzaldehyde nitrogen mustard. The authors hope to make use of tumor tissue with lower pH than normal tissues