Journal of Medicinal Chemistry p. 1547 - 1550 (1986)
Update date:2022-08-03
Topics:
Thurston, Lee S.
Irie, Hiroshi
Tani, Shohei
Han, Fu-Sheng
Liu, Zong-Chao
et al.
It has been reported that the action of etoposide (VP-16) (14) as an antitumor agent is mediated through its interaction with DNA topoisomerase II which results in DNA breakage inside the cell.In order to understand the mechanism of action as well as structure-activity relationships of 14, several novel, synthetic and some naturally occurring analogues related to podophyllotoxin were examined for inhibition of the DNA topoisomerase II activity.Compound 2 exhibited enhanced activity and compound 5 slightly diminished activity relative to 14.A 4β-substituted ether at the C ring and O-demethylation at the E ring appear to enhance activity.
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