首页|NIR imaging human telomeric dimeric G-quadruplexes by malachite green dimers and their antitumor activity
NIR imaging human telomeric dimeric G-quadruplexes by malachite green dimers and their antitumor activity
扫码查看
点击上方二维码区域，可以放大扫码查看
原文链接
NSTL
Elsevier
Though a small number of binders and probes towards human telomeric multimeric G-quadruplexes have been reported to use the tumor detection and therapy in recent years, their detection in visible region and medium antitumor activity limit the development in the research of antitumor drugs. Here, three new malachite green (MG) dimers 1a~c with the different-length polyether linkers have been synthesized to study their NIR visualization towards human telomeric dimeric G-quadruplexes (G2T1) and antitumor activity. The linkers of these dimers could optimize the imaging and binding selectivity for G2T1. Dimer 1c with the longest polyether linker showed higher binding and stabilization towards G2T1 over monomeric G-quadruplexes and ds DNA. More importantly, dimer 1c exhibited selective NIR imaging towards G2T1 in vitro and in cells. In addition, dimer 1c also showed excellent cytotoxicity (IC50 < 1.0 mu M). This study is one of the few research reports on G2T1 probes combined with NIR imaging and the excellent antitumor activity. It gives us to provide a new idea to develop the antitumor drugs with high efficiency and the less side effect by controlling the drug delivery under the guidance of NIR imaging towards G2T1.
Malachite green dimersHuman telomeric dimeric G-quadruplexesNIR imagingAntitumor activityBINDING-PROPERTIESDNACOMPLEXESMULTIMERSDUPLEXCELLS
NSTL
Elsevier
