Amide derivatives of ethacrynic acid: synthesis and evaluation as antagonists of Wnt/beta-catenin signaling and CLL cell survival.

Bioorganic & Medicinal Chemistry Letters
Guangyi JinHoward B Cottam

Abstract

A series of amides of ethacrynic acid was prepared and evaluated for their ability to inhibit Wnt signaling and decrease the survival of CLL cells. Several of the most potent derivatives were active in the low micromolar range. Reduction of the alpha,beta-unsaturated carbon-carbon double bond of EA abrogated both the inhibition of Wnt signaling as well as the decrease in CLL survival. Preliminary mechanism of action studies suggest that these derivatives covalently modify sulfhydryl groups present on transcription factors important for Wnt/beta-catenin signaling.

References

Aug 28, 2007·Journal of Pharmacological Sciences·Fumi Takahashi-Yanaga, Toshiyuki Sasaguri

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Citations

Apr 7, 2010·Proceedings of the National Academy of Sciences of the United States of America·Raymond P WuDennis A Carson
Jul 27, 2011·Proceedings of the National Academy of Sciences of the United States of America·Desheng LuDennis A Carson
Sep 29, 2012·Current Pharmaceutical Design·Andrey Voronkov, Stefan Krauss
May 25, 2010·Epigenomics·Farahnaz B RahmatpanahCharles W Caldwell
Jan 1, 2011·Leukemia Research and Treatment·S ThanendrarajanI G H Schmidt-Wolf
Dec 17, 2015·Future Medicinal Chemistry·Shilong ZhengGuangdi Wang
Aug 7, 2013·Journal of Receptor and Signal Transduction Research·Palani Kirubakaran, Muthusamy Karthikeyan
Jul 20, 2016·Cancers·Kamal AhmedVladimir L Katanaev
Jul 29, 2017·British Journal of Pharmacology·Yung LyouMarian L Waterman
Feb 6, 2020·The Journal of Pharmacology and Experimental Therapeutics·Liang ZhouDesheng Lu

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