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引言由梅泽浜夫及其同事在1966年发现的博莱霉素多年来受到人们极大的关注。独特的分子药理、临床药理、毒理特征及重要的临床作用导致努力发展有效的同系物。目前已报道了300多种博莱霉素同系物。这些同系物可分为三代。最初分离的13种博莱霉素可认为是第一代衍生物。第二代同系物与最初的博莱霉素的不同仅在末端胺结构的改变或在博莱霉素酸分子部分有很小改变的那些化合物。在博莱霉素酸分子部分与博莱霉素有明显不同的则可认为是第三代同系物。塔利索霉素(Tallysomycin)是第三代博莱霉素同系物。已制定出发展博莱霉素同系物的各种计
Introduction Bleomycin, discovered by Mizawa Hamam and colleagues in 1966, has drawn great attention for many years. Unique molecular pharmacology, clinical pharmacology, toxicological traits and important clinical roles have led to efforts to develop effective homologs. More than 300 species of bleomycin homologues have been reported. These homologs can be divided into three generations. The first 13 bleomycin isolates were considered first generation derivatives. The second generation homologues differ from the original bleomycin for only those compounds whose terminal amine structure is altered or which have minor changes in the zeocin molecule moiety. In the bleomycin molecule part and bleomycin have significant differences can be considered as third generation homologues. Tallysomycin is the third generation bleomycin homologue. Various programs have been developed to develop homologues of bleomycin