抗肿瘤剂——CLI。戊二酸双（土木香内酯基）酯和戊二酸双（异土木二醛-B）酯，人类DNA拓扑异构酶II的强效抑制剂。
Antitumor agents--CLI. Bis(helenalinyl)glutarate and bis(isoalantodiol-B)glutarate, potent inhibitors of human DNA topoisomerase II.
作者信息
Chen C H, Yang L M, Lee T T, Shen Y C, Zhang D C, Pan D J, McPhail A T, McPhail D R, Liu S Y, Li D H
机构信息
Natural Products Laboratory, Division of Medicinal Chemistry and Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill 27599.
出版信息
Bioorg Med Chem. 1994 Feb;2(2):137-45. doi: 10.1016/s0968-0896(00)82008-8.
Evaluation of a number of cytotoxic antitumor sesquiterpene lactones and their derivatives has led to the discovery of bis(helenalinyl)glutarate (4) and bis(isoalantodiol-B)glutarate (10) as potent inhibitors of human-derived topoisomerase II. Unlike etoposide, which inhibits by preventing the DNA rejoining process, compounds 4 and 10 inhibit topoisomerase II without causing DNA breakage. The structure-activity relationships of 4, 10, and related compounds are discussed.
对多种细胞毒性抗肿瘤倍半萜内酯及其衍生物的评估，促成了戊二酸双（海伦内酯基）酯（4）和戊二酸双（异土木香二醇-B）酯（10）作为人源拓扑异构酶II的有效抑制剂的发现。与依托泊苷通过阻止DNA重新连接过程发挥抑制作用不同，化合物4和10抑制拓扑异构酶II但不会导致DNA断裂。讨论了化合物4、10及相关化合物的构效关系。
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