Shi Yunlong, Moazami Yasamin, Pierce Joshua G
Department of Chemistry, NC State University, Raleigh, NC 27695, United States.
Department of Chemistry, NC State University, Raleigh, NC 27695, United States; Comparative Medicine Institute, NC State University, Raleigh, NC 27695, United States.
Bioorg Med Chem. 2017 Jun 1;25(11):2817-2824. doi: 10.1016/j.bmc.2017.03.015. Epub 2017 Mar 12.
The pentacyclic guanidinium alkaloids (PGAs) are a family of marine natural products that possess a polycyclic guanidine-containing core and a long alkyl chain tethered spermidine-derived tail that is rarely observed in other natural products. These natural products exhibit potent activities on a wide range of organisms and therefore have attracted the attention of many synthetic chemists; however, the structure-activity relationships and mechanisms of action of PGAs remain largely elusive. Herein we summarize the structure, synthesis, toxicity and mechanisms of action of PGAs and highlight their potential as chemical probes and/or therapeutic leads.
五环胍生物碱(PGAs)是一类海洋天然产物,其具有含多环胍的核心结构以及一条由亚精胺衍生而来的长烷基链尾巴,这种结构在其他天然产物中很少见。这些天然产物对多种生物体表现出强大的活性,因此吸引了众多合成化学家的关注;然而,PGAs的构效关系和作用机制在很大程度上仍不清楚。在此,我们总结了PGAs的结构、合成、毒性和作用机制,并强调了它们作为化学探针和/或治疗先导物的潜力。