摘要
微生物来源的苯并二吡咯类抗生素包括 DUM- A、CC- 10 6 5、Pyrindam ycin、DU M- SA、Gilvusmycin等五类9个 ,它们具有新颖的结构 ,通过分子中独特的药效基团——环丙烷基团与 DNA发生特异性共价结合 ,使 DNA链更稳定 ,从而抑制其解旋 ,达到抗肿瘤的目的。综述这类药物的结构、抗肿瘤活性、作用机制、毒性以及结构改造 ,它们是迄今为止抗瘤活性最强烈的抗生素之一。
Benzodipyrrole antibiotics from Streptomyces, including DUM A, Pyrindamycin, DUM SA, CC 1065,Gilvusmycin et al, possess same pharmacophore, which stabilizes DNA helix chains profoundly by the unique covalent binding between the special cyclopropane ring and the N 3 of adenine in the minor groove of DNA. They inhibit the distortion of DNA, thus showing the strong antitumor activity. The most remarkable feature of these antibiotics is the efficacy against P388 leukemia. Their structures, antitumor activity, mechanism of action, toxicity and structural modification were reviewed. This sort of drugs is one of the most potent antitumor antibiotics.
出处
《药学进展》
CAS
2002年第4期193-198,共6页
Progress in Pharmaceutical Sciences
