Laboratory of Pharmaceutical Design and Synthesis, College of Sciences, Northwest A&F University, Yangling, China.
Bioorg Med Chem Lett. 2010 Sep 1;20(17):5009-12. doi: 10.1016/j.bmcl.2010.07.050. Epub 2010 Jul 16.
In continuation of our program aimed at the discovery and development of natural products-based insecticidal agents, 16 novel 4alpha-alkyloxy-2-chloropodophyllotoxin derivatives were semisynthesized from podophyllotoxin, and preliminarily evaluated for their insecticidal activity against the pre-third-instar larvae of Mythimna separata Walker in vivo. Among all the tested derivatives, especially compounds 4b, 4e, 4g, and 4p exhibited more promising and pronounced insecticidal activity than toosendanin, a commercial insecticide derived from Melia azedarach. Generally, it was obviously demonstrated that the length of straight-chain or branched-chain alkyloxy, and heteroatom-containing cycloalkyloxy at the C-4 position of 2-chloropodophyllotoxin were very important for the insecticidal activity.
在我们旨在发现和开发基于天然产物的杀虫剂的计划的延续中，我们从鬼臼毒素中半合成了 16 种新型 4α-烷氧基-2-氯鬼臼毒素衍生物，并初步评估了它们对三化螟幼虫的体内杀虫活性。在所有测试的衍生物中，特别是化合物 4b、4e、4g 和 4p，表现出比从苦楝树中提取的商业杀虫剂川楝素更有希望和更显著的杀虫活性。一般来说，明显表明 2-氯鬼臼毒素 C-4 位上的直链或支链烷氧基以及含杂原子的环烷氧基的长度对杀虫活性非常重要。
