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近年,在微生物代谢产物的探索研究中,发现了许多新抗癌抗生素,其中最引人注目的是1985年前后相继发现的具有环状烯二炔结构的新型抗生素,包括Calicheamicin、Esperamicin、Dyne-micin A、Neocarzinostatin、C-1027和Kedarcidin(图1),严格来讲,Neocarzinostatin的发色团不含(Z)-烯二炔结构,但由于其作用方式与前几种相同,故仍然被归人该类.由于这类抗生素(1)具有非常强的抗肿瘤活性,(2)其分子中的共轭环状烯二炔结构在天然化合物中是前所未见的,(3)具有经活化形成芳二游离基,迅速夺取两个来自DNA的氢原子,使DNA断裂的新颖抗癌作用机制(图2)等特住,引起世界关注,正在进行多方面的研究.其中,有关烯炔类模型化合物及有关前药的合成研究已有许多报道,并取得不小
In recent years, many new anti-cancer antibiotics have been found in the exploration and research of microbial metabolites. Among them, the most notable ones are the new type of antibiotics with cyclic alkene structure successively discovered before and after 1985, including Calicheamicin, Esperamicin, Dyne- Strictly speaking, the chromophore of Neocarzinostatin does not contain the (Z) -enediyne structure, but because of its mode of action in the same way as the previous ones, it is still under the control of micins A, Neocarzinostatin, C-1027 and Kedarcidin Since these antibiotics (1) have a very strong antitumor activity, (2) the conjugated cycloalkadiyne structure in their molecule is unprecedented in natural compounds, (3) Activation to form aromatic diradicals, the rapid capture of two hydrogen atoms from DNA, the novel anti-cancer mechanism of DNA fragmentation mechanism (Figure 2) and other special, aroused world attention, many aspects of the ongoing research.Among them, There have been many reports on the synthesis of analogous compounds and related prodrugs, and they have achieved considerable success