Synthesis and evaluation of water-soluble paclitaxel prodrugs.
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.
Feng
Xia
X
Department of Pharmaceutical Engineering, School of Chemical Engineering and Technology, Tianjin University, PR China.
Yuan
Ying-Jin
YJ
Wu
Jin-Chuan
JC
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D003432:Cross-Linking Reagents; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D009374:Neoplasms, Experimental / Q000188:drug therapy; D017239:Paclitaxel / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D011092:Polyethylene Glycols; D011355:Prodrugs / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology*; D012995:Solubility; D013329:Structure-Activity Relationship; D016896:Treatment Outcome; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D003432:Cross-Linking Reagents; D011355:Prodrugs; D011092:Polyethylene Glycols; D017239:Paclitaxel