喹诺酮抗肿瘤活性和构效关系研究进展.pdfVIP

456 Chinese Journal of Pharmaceuticals 2010, 41 6 · · 中国医药工业杂志 ( ) 综述与专论 喹诺酮抗肿瘤活性及构效关系研究进展 * 吕 凯，冯连顺，刘明亮 ，郭慧元 100050 (中国医学科学院北京协和医学院医药生物技术研究所，北京 ) 摘要 ：通过对喹诺酮的N-1 、C-2、C-3、C-6 和 C-7 位等进行结构改造，成功地将其经典的抗菌作用转化为对哺乳动物 的细胞毒性，并筛选出若干具有潜在抗肿瘤活性的化合物，其中有数个候选物已处于临床研究或临床前评价阶段。本文 综述了近年来喹诺酮在抗肿瘤活性及其构效关系、作用机制等方面的研究进展。 关键词：喹诺酮；抗肿瘤活性；构效关系；作用机制；综述 R978 A 1001-8255 2010 06-0456-08 中图分类号： 文献标志码： 文章编号： ( ) Advances of Quinolones as Potent Antitumor Agents and The Structure-activity Relationships .. LU Kai, FENG Lianshun, LIU Mingliang*, GUO Huiyuan Institute of Medical Biotechnology, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050 ( ) ABSTRACT: Numerous quinolones had been designed and synthesized, and their actions had been successfully transformed from antibacterial activity to mammalian cell toxicity through structural modifi cations at the N-1, C-2, C-3, C-6 and C-7 positions. It is noted that some quinolone derivatives which have potent antitumor activity are now under the pre-clinical or clinical trials. This article reviews the advances of quinolones as potent antitumor agents, their structure- activity relationships and related action mechanisms. Key Words: quinolones; antitu