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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。
SinenxanA (SIA) was structurally modified to find new taxanes with good overall performance. Different side chains were introduced into C14 of SIA and its modification, and 21 new paclitaxel analogs were synthesized. The anti-tumor activity of 3 kinds of cancer cells in 15 of them was determined. The activity of these compounds in combination with Paclitaxel comparison, a far cry. This article initially discussed the structure-activity relationship of SIA derivatives.