新型白桦脂酸和白桦脂醇衍生物的合成及抗癌活性。
Synthesis and anticancer activity of novel betulinic acid and betulin derivatives.
机构信息
Biozentrum, Martin-Luther-Universität Halle-Wittenberg, Halle, Germany.
出版信息
Arch Pharm (Weinheim). 2010 Aug;343(8):449-57. doi: 10.1002/ardp.201000011.
A series of novel betulinic acid derivatives 3-11 and betulin derivatives 12-17 were synthesized. The compounds were characterized by the means of (1)H- and (13)C-NMR spectroscopy as well as mass spectrometry. The compounds have been tested on ten tumor cell lines of different histogenic origin. The most active derivatives, containing a chloroacetyl group on C-3 in betulinic acid 9 and C-28 in betulin 15, were up to ten times more cytotoxic and many fold more selective towards tumor cells in comparison to normal cells (fibroblasts) than betulinic acid. Furthermore, compound 15 was found to possess cell growth inhibition even when treated for a short time on anaplastic thyroid cancer cells (SW1736).
合成了一系列新型白桦脂酸衍生物 3-11 和白桦脂衍生物 12-17。通过（1）H 和（13）C-NMR 光谱以及质谱对这些化合物进行了表征。对十种不同组织来源的肿瘤细胞系进行了化合物测试。与白桦脂酸相比，在白桦脂酸 9 的 C-3 和白桦脂 15 的 C-28 上含有氯乙酰基的最活性衍生物 9 和 15 对肿瘤细胞的细胞毒性高出十倍以上，对正常细胞（成纤维细胞）的选择性高出数倍。此外，在短时间处理间变性甲状腺癌细胞（SW1736）时，发现化合物 15 具有细胞生长抑制作用。
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