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

Sulfonamide Inhibitors of ß-Catenin Signaling with Different Output on c-MYC as Anticancer Agents.
ChemMedChem. 2020 Sep 18;:
Authors: Silvestri R, Di Magno L, Di Pastena F, Puxeddu M, La Regina G, Coluccia A, Ciogli A, Manetto S, Maroder M, Canettieri G, Nalli M
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. Here we report inhibitors of  β -catenin signaling of potential therapeutic value as anticancer agents. Compound  14  inhibits the effect on Wnt reporter with IC 50  of 7.0 μM, significantly reduces c-MYC levels, inhibits HCT116 colon cancer cell growth with IC 50  of 20.2  μ M, does not violate the Lipinski and Veber rules and shows predicted Caco-2 and MDCK cell permeability  P app  >500 nm/s. Compound  14  seems to have potential for the development of new anticancer therapies.
PMID: 32946182 [PubMed - as supplied by publisher]

Source: ChemMedChem - September 17, 2020 Category: Chemistry Authors: Silvestri R, Di Magno L, Di Pastena F, Puxeddu M, La Regina G, Coluccia A, Ciogli A, Manetto S, Maroder M, Canettieri G, Nalli M Tags: ChemMedChem Source Type: research