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首页> 外文期刊>Current topics in medicinal chemistry >Chemo-enzymatic transformation of taxanes and their reversal activity towards MDR tumor cells
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Chemo-enzymatic transformation of taxanes and their reversal activity towards MDR tumor cells

机译：紫杉烷类的化学酶转化及其对MDR肿瘤细胞的逆转活性

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摘要

Over 200 derivatives have been obtained through chemo-enzymatic transformation of the taxanes derived from cell cultures of Taxus chinensis. The reversal activity towards MDR tumor cells and cyto-toxicity of most these compounds were evaluated, and several derivatives exhibited powerful MDR reversal activity. The substrate-specificities of the two most important biotransformation reactions??C-7β and 9α hydroxylations, were investigated and preliminarily concluded. In addition, some key intermediates in hypothetically biosynthetic pathway of taxoid were obtained. These results indicate that biotransformation combined with chemical transformation is a powerful approach to structural diversification of natural products, lead compound discovery and the study on the structure activity relationships of the derivatives. Moreover, biotransformation may mimic some steps in biosynthetic pathway of natural products and provide useful hints as to their biogenetic study.
机译：通过对红豆杉细胞培养物中的紫杉烷类进行化学-酶促转化，已经获得了200多种衍生物。评估了大多数化合物对MDR肿瘤细胞的逆转活性和细胞毒性，并且几种衍生物表现出强大的MDR逆转活性。研究并初步总结了两个最重要的生物转化反应——C-7β和9α羟基化的底物特异性。此外，获得了假设的紫杉烷生物合成途径中的一些关键中间体。这些结果表明，生物转化结合化学转化是天然产物结构多样化，先导化合物发现以及衍生物结构活性关系研究的有力途径。而且，生物转化可以模仿天然产物的生物合成途径中的某些步骤，并为它们的生物遗传研究提供有用的提示。

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