新型抗肿瘤紫杉烷类化合物的生物学评价：多西他赛C-7和C-10位取代基的改变
Biological evaluation of new antitumor taxoids: alteration of substitution at the C-7 and C-10 of docetaxel.
作者信息
Li Caihong, Qiu Yatao, Li Xing, Liu Nianjin, Yao Zhiyi
机构信息
College of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 210032, China.
Laboratory of Regenerative Biology, Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510530, China.
出版信息
Bioorg Med Chem Lett. 2014 Feb 1;24(3):855-9. doi: 10.1016/j.bmcl.2013.12.083. Epub 2013 Dec 27.
A series of new docetaxol analogues have been designed and synthesized. And their cytotoxicities against cancer cells have been evaluated by MTT method. Most of these compounds showed selective inhibitions on human cancer cell lines. Among them, compound 8 exhibited higher inhibitory activity than Paclitaxel (Taxol) against several cancer cell lines. This work indicated that appropriate modification at C-7 and C-10 of docetaxel might be a promising approach for this unique class of anticancer compounds.
一系列新型多西他赛类似物已被设计并合成出来。并且通过MTT法评估了它们对癌细胞的细胞毒性。这些化合物中的大多数对人类癌细胞系表现出选择性抑制作用。其中，化合物8对几种癌细胞系表现出比紫杉醇更高的抑制活性。这项工作表明，对多西他赛的C-7和C-10位进行适当修饰可能是这类独特抗癌化合物的一种有前景的方法。
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