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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 26, Number 7
BKCSDE 26(7)
July 20, 2005 

Anti-tumor Activity of Paclitaxel Prodrug Conjugated with Polyethylene Glycol
Keyong Ho Lee*, Yong Jun Chung, Youn-Chul Kim, Seog Jeong Song
Paclitaxel, 7-Polyethylene glycol paclitaxel carbonate, Anti-tumor activity, Toxicity, Watersolubility
The purpose of this study was to develop a method for increasing the solubility of paclitaxel in water to reduce its toxicity and make the drug more feasible for chemotherapy. A series of highly water soluble paclitaxel polyethylene glycol (PEG) esters were synthesized and evaluated for their anti-tumor activity and toxicity. The solubility of 7-polyethylene glycol paclitaxel carbonate 5 was 840 mg/mL and the acute toxicity (LD50) was 286 mg/kg. Because of its reduced toxicity, compound 5 showed a dramatic reduction of tumor volume without any loss of animals in long-term treatment (daily consecutive injections for 15 days).
1079 - 1082
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