Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2020 Dec 3;15(23):2264-2268.
doi: 10.1002/cmdc.202000594. Epub 2020 Oct 14.

Sulfonamide Inhibitors of β-Catenin Signaling as Anticancer Agents with Different Output on c-MYC

Laura Di Magno  1 , Fiorella Di Pastena  1 , Michela Puxeddu  2 , Giuseppe La Regina  2 , Antonio Coluccia  2 , Alessia Ciogli  2 , Simone Manetto  2 , Marella Maroder  1 , Gianluca Canettieri  1 , Romano Silvestri  2 , Marianna Nalli  2
Affiliations

Sulfonamide Inhibitors of β-Catenin Signaling as Anticancer Agents with Different Output on c-MYC

Laura Di Magno et al. ChemMedChem. .

Abstract

The Wnt/β-catenin pathway is often found deregulated in cancer. The aberrant accumulation of β-catenin in the cell nucleus results in the development of various malignancies. Specific drugs against this signaling pathway for clinical treatments have not been approved yet. Herein we report inhibitors of β-catenin signaling of potential therapeutic value as anticancer agents. Ethyl 4-((4-(trifluoromethyl)phenyl)sulfonamido)benzoate (compound 14) inhibits the effect on Wnt reporter with an IC50 value of 7.0 μM, significantly reduces c-MYC levels, inhibits HCT116 colon cancer cell growth (IC50 20.2 μM), does not violate Lipinski and Veber rules, and shows predicted Caco-2 and MDCK cell permeability Papp >500 nm s-1 . Compound 14 seems to have potential for the development of new anticancer therapies.

Keywords: c-MYC; colorectal cancer; sulfonamide; β-catenin.

PubMed Disclaimer

References

    1. H. Clevers, K. M. Loh, R. Nusse, Science 2014, 346, 1248012.1-7.
    1. H. Clevers, R. Nusse, Cell 2012, 149, 1192-1205.
    1. V. S. Li, S. S. Ng, P. J. Boersema, T. Y. Low, W. R. Karthaus, J. P. Gerlach, S. Mohammed, A. J. Heck, M. M. Maurice, T. Mahmoudi, H. Clevers, Cell 2012, 149, 1245-1256.
    1. S. Shang, F. Hua, Z.-W. Hu, Oncotarget 2017, 8, 33972-33989.
    1. T. Fevr, S. Robine, D. Louvard, J. Huelsken, Mol. Cell. Biol. 2007, 27, 7551-7559.

Publication types

MeSH terms

LinkOut - more resources