科研之友
微信
新浪微博
Facebook
分享链接
摘要
G-Quadruplex (G4) structures in guanine-rich oligonucleotides are involved in replication, transcription and translation processes in cells, and G4 dysfunction is associated with various diseases. Since G4 stabilization is believed to induce growth inhibition, senescence or apoptosis of cancer cells, various G4-stabilizing agents (G4 ligands) have been synthesized, including our recently developed series of macrocyclic polyoxazoles (OTDs). Among OTD derivatives, those bearing side-chain functional groups that interact with phosphate of the DNA backbone show potent G4-stabilizing ability. Here, we report synthesis of a new macrocyclic hexaoxazole bearing two catechol side chains, i.e., D2H4-6M(4)OTD, based upon our previously reported procedure. D2H4-6M(4)OTD showed moderate and selective stabilizing ability towards G4-forming oligonucleotides without altering their topology. It also showed moderate growth-inhibitory activity towards several cancer cell lines.
- 出版日期2016-2-1
