| 초록 |
Paclitaxel(TaxolⓇ), a natural diterpene isolated from the bark of Taxus brevifolia, is one of the most effective antitumor agents for the treatment of various human solid tumors. It is highly lipophilic and poor solubility in water. We have developed the water-soluble paclitaxel based on PEG conjugates with a newly developed self-immolating linker based on succinic acid and investigated the interaction of water-soluble paclitaxel conjugate and serum proteins. Fluorescent analogues of drugs, with a high quantum yield, are widely used as important tools in studies of the elucidation of structures of drug binding to proteins. The fluorescent water-soluble paclitaxel was synthesized by a condensation reaction of pegylated paclitaxel with 1-pyrene butyric acid etc. These synthesized compounds were characterized by fluorescence spectrometry etc. It could thus be used for the in-vivo study of bioactivities and the efficacy of paclitaxel. |
