一种O-糖基化多西他赛类似物的半合成
Semi-synthesis of an O-glycosylated docetaxel analogue.
作者信息
Nikolakakis Anastasia, Haidara Khadidja, Sauriol Françoise, Mamer Orval, Zamir Lolita O
机构信息
Human Health Research Center, INRS-Institut Armand-Frappier, Université du Québec, 531 Boulevard des Prairies, Laval, Québec, Canada H7V 1B7.
出版信息
Bioorg Med Chem. 2003 Apr 3;11(7):1551-6. doi: 10.1016/s0968-0896(02)00607-7.
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.
一种7β - O - 糖基化多西他赛类似物由9 - 二氢 - 13 - 乙酰基浆果赤霉素III半合成，9 - 二氢 - 13 - 乙酰基浆果赤霉素III是从加拿大红豆杉针叶中分离得到的最丰富的紫杉烷。根据微管蛋白测定，它显示出比紫杉醇更高的生物活性。在MCF7细胞系细胞毒性测定中，与紫杉醇相比，其效力有所降低，但它对耐药细胞系MCF7 - ADR表现出更好的活性。此外，C - 7位上一个糖部分的存在使水溶性相对于紫杉醇增加了一倍。
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