摘要
对烯二炔类抗生素的来源、结构及近年来的有关人工合成、分子设计等方面的新进展进行综述。烯二炔类抗生素是一种有着全新结构的高效抗肿瘤抗生素,其结构中含有双烯双炔Bergman共轭大环,通过形成苯型游离基的方式直接氧化破坏肿瘤细胞DNA分子链,具有抗瘤谱广、强生物活性和作用机制独特的特点。
The enediyne antitumor antibiotics , such as esperamicin, calicheamicin, dynemicin, lindamicin, kedarcidin, shishijimicins A-C families have aroused considerable interest owing to their exceptional potency, the potent inhibitory activity against a wide range of tumor cells, the unique structure of their 1,5-diyne-3-ene core, and their intriguing mode of action. The key mechanism of activation of these compounds toward DNA cleavage was a Bergman cyclization of the enediyne core triggered by an intramolecular conjugate. The advance in researches of enediyne antibiotics has been described, including the novel antibiotics from mircoorganisms, chemical synthesis and drug molecular design on abroad recently.
出处
《药学进展》
CAS
2005年第10期433-439,共7页
Progress in Pharmaceutical Sciences
