Ma Da-You, Wang Long-Long, Lai Qin, Peng Kun-Jian, Li Xuan, Li Zeng-Xia, Liu Li-Jun, Luo Zhi-Yong, Liu Su-You
School of Pharmaceutical Sciences, Central South University, Changsha 410013, China.
School of Pharmaceutical Sciences, Central South University, Changsha 410013, China.
Bioorg Med Chem Lett. 2018 Nov 1;28(20):3346-3349. doi: 10.1016/j.bmcl.2018.09.005. Epub 2018 Sep 5.
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.
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型多杀菌素衍生物。部分衍生物对受试人癌细胞系显示出显著增强的抗增殖能力。构效关系研究表明，亲脂性对这些衍生物的抗增殖作用有很大影响。活性最强的化合物11d比多杀菌素A表现出显著增强的氧化磷酸化抑制和凋亡诱导能力。
