Paclitaxel derivatives for targeted therapy of cancer: toward the development of smart taxanes.

@article{Safavy1999PaclitaxelDF,
  title={Paclitaxel derivatives for targeted therapy of cancer: toward the development of smart taxanes.},
  author={Ahmad Safavy and Kevin P. Raisch and Mohammad B Khazaeli and Donald J Buchsbaum and James A. Bonner},
  journal={Journal of medicinal chemistry},
  year={1999},
  volume={42 23},
  pages={4919-24}
}
The pharmacologic efficacy of the promising antitumor agent paclitaxel (Taxol) may be potentially enhanced through derivatization of the drug to a water-soluble tumor-recognizing conjugate. This work reports the design and synthesis of the first tumor-directed derivative of paclitaxel. A 7-amino acid synthetic peptide, BBN[7-13], which binds to the cell surface bombesin/gastrin-releasing peptide (BBN/GRP) receptor, was conjugated to the paclitaxel-2'-hydroxy function by a heterobifunctional… CONTINUE READING

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