肿瘤化学治疗药物的研究——9-肼基吖啶衍生物的合成

吖啶衍生物能优先地与活细胞的核酸相结合,早为人们所知。它在抗肿瘤作用的开发方面,波兰Ledochowski和新西兰Cain及同工者做了大量工作。Peck和Baguley等指出:9-脂胺基和9-苯胺基吖啶类结构中吖啶色基是药物与DNA的结合部分,药物抗肿瘤和致突变作用,跟吖啶色基与DNA结合的亲和性紧密相关,若在吖啶色基上连接一些大基团,降

STUDY ON TUMOR CHEMOTHERAPEUTIC AGENTS:SYNTHESIS OF 9-HYDRAZINOACRIDINE DERIVATIVES

Twenty-nine hydrazones, amido and imido-type compounds of 9-hydrazinoacridine (9-hydrazonoacridines and 9-acylhydrazinoacridines) were prepared. The 9-acylhydrazinoacridines were obtained from the corresponding acylating agents and 9-hydrazinoacridine by condensation under suitable conditions, Results of animal screening of 9-hydrazonoacridines showed compound 1 to be effective against mouse S_(180) and marginal active on mouse U_(14). Compound 6 exhibited activity against hepatoma (solid) in mice. Studies on antitumor actions of the 9-acylhydrazinoacridines are in progress.