Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, West Lafayette, Indiana 47907, United States.
Org Lett. 2012 Aug 17;14(16):4038-41. doi: 10.1021/ol300683r. Epub 2012 Aug 2.
A set of synthetic approaches were developed and applied to the synthesis of eight frame-shifted farnesyl diphosphate (FPP) analogs. These analogs bear increased or decreased methylene units between the double bonds and/or diphosphate moieties of the isoprenoid structure. Evaluation versus mammalian FTase revealed that small structural changes can lead to dramatic changes in substrate ability.
开发了一套综合方法,并将其应用于合成 8 种移位法呢基二磷酸(FPP)类似物。这些类似物在异戊二烯结构的双键和/或二磷酸部分之间具有增加或减少的亚甲基单元。与哺乳动物 FTase 的评估表明,小的结构变化可能导致底物能力的显著变化。