In order to enhance the mitochondria-targeting ability of spinosad. A series of quartenary ammonium spinosyn derivatives was designed and synthesized. Some of the derivatives displayed greatly enhanced antiproliferative ability towards tested human cancer cell lines. The structure activity relationship study indicated that lipophilicity has a great influence on the antiproliferative effects of these derivatives. The most active compound 11d exhibited remarkably enhanced OXPHS inhibition and apoptosis inducing ability than spinosyn A.

中文翻译：

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新型季铵基多杀菌素衍生物的合成及抗增殖活性

为了增强多杀菌素的线粒体靶向能力。设计并合成了一系列季铵基多杀菌素衍生物。一些衍生物显示出对测试的人类癌细胞系极大的增强的抗增殖能力。结构活性关系研究表明，亲脂性对这些衍生物的抗增殖作用有很大影响。活性最高的化合物11d比Spinosyn A表现出显着增强的OXPHS抑制和凋亡诱导能力。