AI Article Synopsis
- Two new binaphthyl amines were created using key chemistry techniques, specifically Buchwald amination and oxidative homocoupling.
- One of the compounds, featuring two triazole rings, binds strongly to the c-MYC G-quadruplex, triggers a fluorescence response, and successfully stains cell nuclei.
- Both compounds demonstrate cancer-fighting potential by causing cell cycle arrest and apoptosis in cancer cells while also reducing c-MYC expression at both transcriptional and translational levels.
Article Abstract
Two novel binaphthyl amines have been designed and synthesized using Buchwald amination and oxidative homocoupling as key steps. The binaphthyl amine containing two triazole rings shows higher affinity for c-MYC G-quadruplex, exhibits fluorescence "turn-on" response with c-MYC, and stains the nucleus in cells. The triazolyl binaphthyl amine shows cytotoxicity for cancer cells by inducing G2/M phase cell cycle arrest and apoptosis. Moreover, both ligands can downregulate c-MYC expression at transcriptional and translational levels.
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| http://dx.doi.org/10.1021/acs.jmedchem.6b00328 | DOI Listing |
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