黄光燕, 郭积玉, 梁晓天. 紫杉烷类化合物 SINENXAN A 的结构修饰及其衍生物的构效关系研究J. 药学学报, 1998, 33(8): 576-586.
引用本文: 黄光燕, 郭积玉, 梁晓天. 紫杉烷类化合物 SINENXAN A 的结构修饰及其衍生物的构效关系研究J. 药学学报, 1998, 33(8): 576-586.
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Huang Guangyan, Guo Jiyu , Liang Xiaotian, . STUDIES ON STRUCTURE MODIFICATION AND STRUCTURE-ACTIVITY RELATIONSHIP OF NEW TAXOIDS DERIVED FROM SINENXAN AJ. Acta Pharmaceutica Sinica, 1998, 33(8): 576-586.
Citation: Huang Guangyan, Guo Jiyu , Liang Xiaotian, . STUDIES ON STRUCTURE MODIFICATION AND STRUCTURE-ACTIVITY RELATIONSHIP OF NEW TAXOIDS DERIVED FROM SINENXAN AJ. Acta Pharmaceutica Sinica, 1998, 33(8): 576-586.
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紫杉烷类化合物 SINENXAN A 的结构修饰及其衍生物的构效关系研究

STUDIES ON STRUCTURE MODIFICATION AND STRUCTURE-ACTIVITY RELATIONSHIP OF NEW TAXOIDS DERIVED FROM SINENXAN A

    摘要
  • 摘要: 为寻找新的综合性能好的紫杉烷类化合物,对sinenxanA(SIA)进行结构修饰。在SIA及其修饰物的C14位引入不同的的侧链,共合成新的紫杉醇类似物21个,对其中的15个化合物进行了3种癌细胞的体外抗肿瘤活性测定,这些化合物的活性与紫杉醇比较,相差甚远。本文初步讨论了SIA衍生物的构效关系。

     

    Abstract: In order to develop new taxol analogues with possible antitumor properties, sinenxan A (SIA), a new biosynthetic taxoid, was chemically modified, mainly by esterification of C14-OH with taxol-like side-chain acids. Twenty-one new taxoids thus formed were tested on three kinds of cell lines. Their activities are far below those of taxol. The SAR of SIA derivatives partly agree with that of taxol and can be roughly discerned.

     

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