In 2018,Shaw, Scott K.; Liu, Wenqi; Gomez Duran, Cesar Fernando Azael; Schreiber, Cynthia L.; de Lourdes Betancourt Mendiola, Maria; Zhai, Canjia; Roland, Felicia M.; Padanilam, Simon J.; Smith, Bradley D. published 《Non-Covalently Pre-Assembled High-Performance Near-Infrared Fluorescent Molecular Probes for Cancer Imaging》.Chemistry – A European Journal published the findings.Electric Literature of C30H30N10 The information in the text is summarized as follows:
New fluorescent mol. probes, which can selectively target specific cell surface receptors, are needed for microscopy, in vivo imaging, and image guided surgery. The preparation of multivalent probes using standard synthetic chem. can be a laborious process due to low reaction yields caused by steric effects. In this study, fluorescent mol. probes were prepared by a programmed non-covalent pre-assembly process that used a near-IR fluorescent squaraine dye to thread a macrocycle bearing a cyclic arginine-glycine-aspartate peptide antagonist (cRGDfK) as a cancer targeting unit. Cell microscopy studies using OVCAR-4 (ovarian cancer) and A549 (lung cancer) cells that express high levels of the integrin αvβ3 or αvβ5 receptors, resp., revealed a multivalent cell targeting effect. That is, there was comparatively more cell uptake of a pre-assembled probe equipped with two copies of the cRGDfK antagonist than a pre-assembled probe with only one appended cRGDfK antagonist. The remarkably high photostability and low phototoxicity of these near-IR probes allowed for acquisition of long-term fluorescence movies showing endosome trafficking in living cells. In vivo near-IR fluorescence imaging experiments compared the biodistribution of a targeted and untargeted probe in a xenograft mouse tumor model. The average tumor-to-muscle ratio for the pre-assembled targeted probe was 3.6 which matches the tumor targeting performance reported for analogous cRGDfK-based probes that were prepared entirely by covalent synthesis. The capability to excite these pre-assembled near-IR fluorescent probes with blue or deep-red excitation light makes it possible to determine if a target site is located superficially or buried in tissue, a probe performance feature that is likely to be very helpful for eventual applications such as fluorescence guided surgery. In the experiment, the researchers used Tris((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)amine(cas: 510758-28-8Electric Literature of C30H30N10)
Tris((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)amine(cas: 510758-28-8) can stabilizes Cu(I) towards disproportionation and oxidation thus enhancing its catalytic effect in the azide-acetylene cycloaddition.Electric Literature of C30H30N10Polytriazolylamines were synthesized by the copper(I)-catalyzed ligation of azides and alkynes.
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics