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Synthesis and evaluation of water-soluble paclitaxel prodrugs
Xia Feng1, Ying-Jin Yuan, Jin-Chuan Wu
1Department of Pharmaceutical Engineering, School of Chemical Engineering and Technology, Tianjin University, PR China.
Bioorganic & Medicinal Chemistry Letters
|October 24, 2002
Abstract:
A series of water-soluble 2'-paclitaxel prodrugs were synthesized by attaching paclitaxel to polyethylene glycol (PEG) through amino acid spacers. The prodrugs showed highly improved water solubility, enhanced in vitro cytotoxicity and in vivo antitumor activity compared with the native drug, paclitaxel.