Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Bioorg Med Chem Lett. 2010 Sep 1;20(17):5104-7. doi: 10.1016/j.bmcl.2010.07.023. Epub 2010 Jul 11.
Synthesis and biological evaluation of jasplakinolide analogs are described. The synthesis of analogs utilized a diastereoselective syn-aldol reaction and an orthoester Claisen rearrangement as key steps. All synthetic analogs were evaluated for their ability to disrupt the actin cytoskeleton. Compounds 2, 3, and 4 essentially displayed similar activity to jasplakinolide.
本文描述了 Jasplakinolide 类似物的合成和生物评价。类似物的合成利用了非对映选择性 syn-aldol 反应和邻酯 Claisen 重排作为关键步骤。所有合成的类似物都评估了它们破坏肌动蛋白细胞骨架的能力。化合物 2、3 和 4 基本上表现出与 Jasplakinolide 相似的活性。
