Synthesis and biological evaluation of novel neamine-nucleoside conjugates potentially targeting to RNAs
Eighteen novel neamine-nucleoside conjugates with ethylenediamine-lysine or ethylenediamine-argi-nine as the linker were synthesized and their potential binding to A site of 16S RNA and TAR RNA was evaluated using SPR (surface plasmon resonance). Compared with neamine, compounds 10i and 10q show 63 and 4.8 times potential in binding to A site of 16S RNA and eight and six times potential in binding to TAR RNA, respectively. According to the data of SPR, it indicates that amino acid residue and nucleobase moieties of the designed neamine-nudeosides conjugates exhibit the important contributions for the binding to A site of 16S RNA and TAR RNA. The molecular docking study on the interaction between the ligands and A site of 16S RNA is in agreement with the experimental data. The novel type of modification may provide a promising way for the development of neamine derivatives effectively targeting to RNAs.
Yanli Xu Hongwei Jin Zhenjun Yang Liangren Zhang Lihe Zhang
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University 100191, Beijing, China
国际会议
武汉
英文
108-119
2010-09-01（万方平台首次上网日期，不代表论文的发表时间）