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http://dx.doi.org/10.5012/bkcs.2005.26.7.1079

Anti-tumor Activity of Paclitaxel Prodrug Conjugated with Polyethylene Glycol  

Lee, Keyong-Ho (Kolon Central Research Park)
Chung, Yong-Jun (Kolon Central Research Park)
Kim, Youn-Chul (Kolon Central Research Park)
Song, Seog-Jeong (Kolon Central Research Park)
Publication Information
Bulletin of the Korean Chemical Society / v.26, no.7, 2005 , pp. 1079-1082 More about this Journal
Abstract
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 ($LD_{50}$) 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).
Keywords
Paclitaxel; 7-Polyethylene glycol paclitaxel carbonate; Anti-tumor activity; Toxicity; Watersolubility;
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