Antitumor agents. 111. New 4-hydroxylated and 4-halogenated anilino derivatives of 4'-demethylepipodophyllotoxin as potent inhibitors of human DNA topoisomerase II.

@article{Lee1990AntitumorA1,
  title={Antitumor agents. 111. New 4-hydroxylated and 4-halogenated anilino derivatives of 4'-demethylepipodophyllotoxin as potent inhibitors of human DNA topoisomerase II.},
  author={Kiho Lee and S A Beers and Masayuki X. Mori and Zhi- Qiang Wang and Yao Haur Kuo and Liang Li and Stephen Y Liu and J Y Chang and F S Han and Yu Chin Cheng},
  journal={Journal of medicinal chemistry},
  year={1990},
  volume={33 5},
  pages={1364-8}
}
A series of C-4 hydroxylated and halogenated anilino derivatives of epipodophyllotoxin or 4'-demethylepipodophyllotoxin have been synthesized and evaluated for their inhibitory activity against the human DNA topoisomerase II as well as for their activity in causing cellular protein-linked DNA breakage. Compounds 11-17 and 22 are more potent than etoposide in causing DNA breakage, while compounds 11-13, 15, 16, and 20 are as active or more active than etoposide in their inhibition of the human… CONTINUE READING