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在过去十二年中,已有四种含有烯二炔亚单位的天然抗癌抗生素dynemicin A,cali-cheamicin Υ_1,esperamicin A_1,neocarzi-nostatin从细菌中分离出来。这些化合物都具有显著的抗癌活性。与那些通过链内交联的形成而破坏细胞核DNA的烷化剂不同,这些新的化合物能通过代谢形成很活泼的双自由基从DNA的糖磷酸酯骨架上夺取氢原子。这些天然抗癌药分子的整体结构都有一个烯二炔单位,一个运载系统(糖或嵌入基)和一个引发机构。这些分子实际上是前体药物,在引发前,2个三键被隔开。
In the past 12 years, four natural anticancer antibiotics, dynemicin A, cali-cheamicin Y1, esperamicin A_1, neocarzi-nostatin, containing enediyne subunits have been isolated from bacteria. These compounds all have significant anticancer activity. Unlike alkylating agents that disrupt nuclear DNA by the formation of intra-chain cross-links, these new compounds can take hydrogen atoms from the sugar-phosphate backbone of DNA by metabolizing to form very reactive diradicals. The overall structure of these natural anti-cancer drug molecules has an enediyne unit, a delivery system (sugar or embedded groups) and a trigger mechanism. These molecules are actually prodrugs, and two triple bonds are separated before priming.