Department of Chemistry and Biology "A. Zambelli", University of Salerno, Via Giovanni Paolo II, 132, Fisciano (SA) 84084, Italy.
Org Biomol Chem. 2018 Sep 19;16(36):6708-6717. doi: 10.1039/c8ob01522h.
Five new cyclic peptoids containing (2S,4R)-4-hydroxyproline (Hyp) residues have been designed and synthesized using a mixed "submonomer/monomer" approach. Alkali metal cation affinities and ion transport activities were assessed by experimental (NMR and HPTS assay in liposomes) and computational methods. Easy functionalization of hydroxyproline residues afforded a bouquet of cyclic oligomers showing correlation between ion transport abilities and cytotoxic activities on selected human cancer cell lines.
已经设计并合成了五个含有（2S,4R）-4-羟基脯氨酸（Hyp）残基的新型环状肽。通过实验（NMR 和脂质体中的 HPTS 测定）和计算方法评估了碱金属阳离子亲和力和离子传输活性。脯氨酸残基的易于功能化提供了一系列环状低聚物，显示了在选定的人类癌细胞系上离子传输能力和细胞毒性活性之间的相关性。
