Orally active docetaxel analogue: synthesis of 10-deoxy-10-C-morpholinoethyl docetaxel analogues.

@article{Iimura2001OrallyAD,
  title={Orally active docetaxel analogue: synthesis of 10-deoxy-10-C-morpholinoethyl docetaxel analogues.},
  author={Shin Iimura and Kouichi Uoto and Satoru Ohsuki and Jun Chiba and Tetsuya Yoshino and Michio Iwahana and Takeshi Jimbo and Hirofumi Terasawa and Tsunehiko Soga},
  journal={Bioorganic & medicinal chemistry letters},
  year={2001},
  volume={11 3},
  pages={407-10}
}
To improve cytotoxicity of 10-deoxy-10-C-morpholinoethyl docetaxel analogues against various tumor cell lines including resistant cells expressing P-glycoprotein (P-gp), we modified the 7-hydroxyl group to hydrophobic groups (methoxy, deoxy, 6,7-olefin, alpha-F, 7-beta-8-beta-methano, fluoromethoxy). Among these analogues, the 7-methoxy analogue showed the… CONTINUE READING