Xu Hui, Xiao Xiao
Laboratory of Pharmaceutical Design and Synthesis, College of Life Sciences, Northwest A&F University, Yangling 712100, China.
Bioorg Med Chem Lett. 2009 Sep 15;19(18):5415-8. doi: 10.1016/j.bmcl.2009.07.116. Epub 2009 Jul 28.
By using podophyllotoxin as a lead compound, eight novel esters of 2-chloropodophyllotoxin were designed, semisynthesized, and preliminarily evaluated for their insecticidal activity against the pre-third-instar larvae of Mythimna separata Walker in vivo for the first time. Among all the tested compounds, especially three esters of 2-chloropodophyllotoxin 8a, 8c, and 8g, and one intermediate 6 showed more promising and pronounced insecticidal activity than toosendanin, a commercial insecticide derived from Melia azedarach.
以鬼臼毒素为先导化合物，首次设计、半合成了8种新型2-氯鬼臼毒素酯，并对其对粘虫（Mythimna separata Walker）三龄前幼虫的体内杀虫活性进行了初步评价。在所有测试化合物中，尤其是2-氯鬼臼毒素的三种酯8a、8c和8g，以及一种中间体6，表现出比从苦楝中提取的商业杀虫剂川楝素更有前景和更显著的杀虫活性。
