Chauhan, Ajay ; Paul, Rakesh ; Debnath, Manish ; Bessi, Irene ; Mandal, Samir ; Schwalbe, Harald ; Dash, Jyotirmayee (2016) Synthesis of Fluorescent Binaphthyl Amines That Bind c-MYC G-Quadruplex DNA and Repress c-MYC Expression Journal of Medicinal Chemistry, 59 (15). pp. 7275-7281. ISSN 0022-2623
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Official URL: http://doi.org/10.1021/acs.jmedchem.6b00328
Related URL: http://dx.doi.org/10.1021/acs.jmedchem.6b00328
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.
Item Type: | Article |
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Source: | Copyright of this article belongs to ResearchGate GmbH. |
ID Code: | 126594 |
Deposited On: | 17 Oct 2022 05:45 |
Last Modified: | 17 Oct 2022 05:45 |
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