- 期刊
喜樹鹼的化學及抗癌構效關係研究之最新進展
Recent Advances in the Chemical and Antitumor Structure-Activity Correlation Studies of Camptothecin
摘要
喜樹鹼(1)係由Wall等於1966年從中國特產的喜樹(Camptotlzeca acuminata )中分離出的抗腫瘤生物鹼。從同植物中分出的10-羥基喜樹鹼已在中國作為抗癌藥物，用於臨床。此外，三種顯示強烈的DNA Topoisomerase I抑制活性的喜樹鹼衍生物，Hycampotamine (Topotecan). 9-aminocamptothecin，及CPT-11，已分別在歐洲、美國、和日本進行臨床試驗中，試用於直腸癌及其他癌症之治療。本文將結合筆者實驗室近年來的研究成果，重點介紹近三四年來對喜樹鹼的基本骨架(A-E環)進行化學改造及構效關係研究之最新進展。
關鍵字
無資料並列摘要
Camptothecin (1) is a potent antitumor alkaloid isolated form the Chinese tree Camptotheca acuminata in 1966. 10- Hydroxycamptothecin isolated from the same plant has been used clinically in China as an anticancer drug. In addition, three derivatives of camptothecin, hycamptamine (Topotecan), 9-aminocamptothecin, and CPT-11, which are potent inhibitors of DNA topoisomerase I, are being tested clinically as anticancer drugs against colon and other cancers in Europe, the USA and Japan, respectively. This review covers the most recent advances in studies dealing with the chemical modification of rings A-E of the basic camptothecin skeleton, as well as structure-activity relationship studies of camptothecin.