高喜树碱是新一代喜树碱类拓扑异构酶Ⅰ抑制剂,它与喜树碱的主要区别是将喜树碱E环的α-羟基-δ-内酯环变为β-羟基-ε-内酯环。高喜树碱的结构修饰与喜树碱类似,主要集中在高喜树碱的7、9、10及20位,从中发现获得了多个高活性化合物,其中化合物BN80915和BN80927分别进入Ⅱ期和Ⅰ期临床研究用于治疗非小细胞肺癌和晚期实体瘤。本文对高喜树碱的研究进展做一综述。 HCPT is a new generation of camptothecin topoisomerase I inhibitors. The main difference between camptothecin and camptothecin is to change the α-hydroxy-δ-lactone ring of camptothecin E ring into β-hydroxy-ε- Lactone ring. High-camptothecin structural modifications similar to camptothecin, mainly in the high camptothecin 7,9,10 and 20, from which we found a number of highly active compounds, compounds BN80915 and BN80927 were entered Phase Ⅱ and Ⅰ clinical studies For the treatment of non-small cell lung cancer and advanced solid tumors. This article reviewed the research progress of high camptothecin.