Kodet John G, Beutler John A, Wiemer David F
Department of Chemistry, University of Iowa, Iowa City, IA 52242-1294, United States.
Molecular Targets Laboratory, Center for Cancer Research, NCI-Frederick, Frederick, MD 21702, United States.
Bioorg Med Chem. 2014 Apr 15;22(8):2542-52. doi: 10.1016/j.bmc.2014.02.043. Epub 2014 Mar 6.
As part of a program to explore the biological activity of analogues of the natural schweinfurthins, a set of compounds has been prepared where an indole system can be viewed as a substitution for the resorcinol substructure of the schweinfurthin's D-ring. Twelve of these schweinfurthin indoles have been prepared and evaluated in the 60 cell line screen of the National Cancer Institute. While a range of activity has been observed, it is now clear that schweinfurthin indoles can demonstrate the intriguing pattern of activity associated with the natural stilbenes. In the best cases, these indole analogues display both potency and differential activity across the various cell lines comparable to the best resorcinol analogues.
作为探索天然施魏因富特菌素类似物生物活性项目的一部分，已制备了一组化合物，其中吲哚系统可视为施魏因富特菌素D环间苯二酚亚结构的替代物。已制备了其中12种施魏因富特菌素吲哚，并在美国国立癌症研究所的60种细胞系筛选中进行了评估。虽然观察到了一系列活性，但现在很明显，施魏因富特菌素吲哚可以表现出与天然芪类化合物相关的有趣活性模式。在最佳情况下，这些吲哚类似物在各种细胞系中表现出的效力和差异活性与最佳间苯二酚类似物相当。
