Camptothecin-20-PEG ester transport forms: the effect of spacer groups on antitumor activity.

@article{Greenwald1998Camptothecin20PEGET,
  title={Camptothecin-20-PEG ester transport forms: the effect of spacer groups on antitumor activity.},
  author={Richard Greenwald and Annapurna Pendri and Charles D. Conover and C Lee and Yun Hui Choe and Carl W. Gilbert and Anthony I. Martinez and Jing Xia and Dechun Wu and M Hsue},
  journal={Bioorganic & medicinal chemistry},
  year={1998},
  volume={6 5},
  pages={551-62}
}
An improved synthesis of the hindered PEG-camptothecin diester transport form has been achieved using the Mukaiyama reagent. We have also assessed the effect of changing the electronic configuration of the (d-position of PEG-camptothecin transport forms on the rates of hydrolysis of the pro-moiety, and attempted to correlate these differences to efficacy in two animal models. In addition to the simple substitution of N for O, other synthetic modifications of these atoms were accomplished by… CONTINUE READING

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