Beyond the Antagonism: Self-Labeled Xanthone Inhibitors as Modeled "Two-in-One" Drugs in Cancer Therapy

ACS Omega
Fu-Chao YuJun Lin

Abstract

Self-labeled inhibitors (SLIs) are promising for creating links, ranging from cancer therapy and metastatic pathways to mechanistic elucidation. In this study, a new category of "two-in-one" fluorescent xanthone inhibitors was developed for the systematic evaluation of anticancer activity and the selective imaging of cytoplasm in vitro. These xanthone inhibitors presented high fluorescent brightness, working over a wide pH range enabled by a "switchable reaction" of the heterocyclic backbone. The strength and nature of fluorescence were probed via spectroscopic methods and density functional theory calculations on the molecular level, respectively. Along with the potent anticancer activity, which was demonstrated using MTT and clonogenic assays with high fluorescent brightness in the cytoplasm, SLI 3fd could be established as a modeled self-monitoring drug in cancer therapy.

References

May 9, 2008·Journal of the American Chemical Society·Craig A ParishGuy Harris
May 24, 2012·Chemical Reviews·Kye-Simeon Masters, Stefan Bräse
Nov 22, 2012·Journal of Medicinal Chemistry·Xiaojin ZhangQidong You
Jan 22, 2013·Natural Product Reports·Dana K WinterJohn A Porco
Dec 23, 2014·Natural Product Reports·Christopher D Donner
Jan 27, 2015·Natural Product Reports·John W BluntMichèle R Prinsep
Mar 5, 2015·Chemical Society Reviews·Sherif I ElshahawiJon S Thorson
Feb 24, 2016·Journal of Natural Products·Aline CoqueiroVanderlan da S Bolzani
Mar 5, 2016·Journal of Medicinal Chemistry·Silvia GobbiAlessandra Bisi
Jul 21, 2016·Chemical Reviews·Laura Nunes SilvaDanielle Silva Trentin
Jul 28, 2016·Journal of the American Chemical Society·Janjira RujirawanichJoseph M Ready
Aug 1, 2013·ChemPlusChem·Debabrata MaityT Govindaraju

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Citations

Apr 13, 2018·The Journal of Organic Chemistry·Cong-Hai ZhangSheng-Jiao Yan

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Methods Mentioned

BETA
nuclear magnetic resonance
X-ray
Assay
NMR

Software Mentioned

Gaussian

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