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Chemo-enzymatic synthesis of ester-linked taxol-oligosaccharide conjugates as potential prodrugs |
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| Authors: | Kei Shimoda Hatsuyuki Hamada |
| Affiliation: | a Department of Pharmacology and Therapeutics, Faculty of Medicine, Oita University, 1-1 Hasama-machi, Oita 879-5593, Japan b National Institute of Fitness and Sports in Kanoya, 1 Shiromizu-cho, Kagoshima 891-2390, Japan c Department of Life Science, Faculty of Science, Okayama University of Science, 1-1 Ridai-cho, Okayama 700-0005, Japan |
| Abstract: | 7-Glycolylpaclitaxel 2″-O-α-glucooligosaccharides, novel taxol (paclitaxel) prodrugs of ester-linked oligosaccharide series compounds, were synthesized by chemo-enzymatic procedures, including enzymatic transglycosylations with α-glucosidase and cyclodextrin glucanotransferase. The water-solubility of 7-glycolylpaclitaxel 2″-O-α-glucopentaoside was 2.7 mM, which was 6.8 thousand-fold higher than that of paclitaxel. C-7 modification of paclitaxel with a longer oligosaccharide chain decreased the in vitro cytotoxicity of paclitaxel against KF human ovarian cancer cells. |
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