Antitumor agents. 100. Inhibition of human DNA topoisomerase II by cytotoxic ether and ester derivatives of podophyllotoxin and alpha-peltatin.

@article{Thurston1989AntitumorA1,
  title={Antitumor agents. 100. Inhibition of human DNA topoisomerase II by cytotoxic ether and ester derivatives of podophyllotoxin and alpha-peltatin.},
  author={L S Thurston and Yasuhiro Imakura and Masao Haruna and Daniel Hsieh-Hsin Li and Zhi Cai Liu and Stephen Y Liu and Yu Chin Cheng and Kuo Hsiung Lee},
  journal={Journal of medicinal chemistry},
  year={1989},
  volume={32 3},
  pages={604-8}
}
A principal mechanism of action of the clinical antitumor drugs etoposide (1) and teniposide (2) is the inhibition of catalytic activity of type II DNA topoisomerase and concurrent enzyme-mediated production of lethal DNA strand breaks. Substitution of the glycosidic moiety of 1 or 2 by ester and ethers, as well as the esterification and etherification of alpha-peltatin (4) including its glucosidic ethylidene and thenylidene cyclic acetals (25 and 26), has afforded compounds of much less… CONTINUE READING