Antitumor agents--CLI. Bis(helenalinyl)glutarate and bis(isoalantodiol-B)glutarate, potent inhibitors of human DNA topoisomerase II.

Journal Article

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.

Full Text

Duke Authors

Cited Authors

  • Chen, CH; Yang, LM; Lee, TT; Shen, YC; Zhang, DC; Pan, DJ; McPhail, AT; McPhail, DR; Liu, SY; Li, DH

Published Date

  • February 1994

Published In

Volume / Issue

  • 2 / 2

Start / End Page

  • 137 - 145

PubMed ID

  • 7922123

Pubmed Central ID

  • 7922123

Electronic International Standard Serial Number (EISSN)

  • 1464-3391

International Standard Serial Number (ISSN)

  • 0968-0896

Digital Object Identifier (DOI)

  • 10.1016/s0968-0896(00)82008-8


  • eng