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  • Title: Semi-synthesis of an O-glycosylated docetaxel analogue.
    Author: Nikolakakis A, Haidara K, Sauriol F, Mamer O, Zamir LO.
    Journal: Bioorg Med Chem; 2003 Apr 03; 11(7):1551-6. PubMed ID: 12628678.
    Abstract:
    A 7beta-O-glycosylated docetaxel analogue was semi-synthesized from 9-dihydro-13-acetylbaccatin III, the most abundant taxane isolated from the needles of Taxus canadensis. It was shown to be more bioactive than paclitaxel according to the tubulin assay. It had a reduced potency in the MCF7 cell line cytotoxicity assay compared to paclitaxel, but it demonstrated better activity against the drug resistant cell line MCF7-ADR. In addition, the presence of one sugar moiety on C-7 doubled the water solubility versus that of paclitaxel.
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