摘要
格尔德霉素是一种苯醌安莎霉素类抗生素,有极强的抗肿瘤活性,其衍生物17AAG(17-丙烯胺-17-去甲氧基格尔德霉素)是格尔德霉素的17位甲氧基被烯丙胺基取代所得,与格尔德霉素相比,其毒性更低,抗癌活性更高。综述17AAG的作用机制、治疗应用、药代动力学、毒性等研究进展。
Geldanamycin is a benzoquinone ansamycin antibiotic with strong anti-tumor activity. Its derivative 17AAG(17-allylamino-17-demethoxy-geldanamycin) is obtained by substituting allylamine for geldanamycin's 17-methoxy, which has shown lower toxicity and higher antitumor activity, compared with geldanamycin.The advances on the mechanism of action, therapeutic use, pharmacokinetics and toxicity of 17 AAG were reviewed.
出处
《药学进展》
CAS
2015年第8期598-602,共5页
Progress in Pharmaceutical Sciences
关键词
17AAG
抗癌抗生素
作用机制
治疗应用
药代动力学
毒性
17-AAG
anticancer antibiotic
mechanism of action
therapeutic use
pharmacokinetics
toxicity