1The Wnt/beta-catenin pathway is often found deregulated incancer. The aberrant accumulation of beta-catenin in the cellnucleus results in the development of various malignancies. Specific drugs against this signaling pathway for clinical treat-ments have not been approved yet. Herein we report inhibitorsof beta-catenin signaling of potential therapeutic value asanticancer agents. Ethyl 4-((4-(trifluoromethyl)phenyl)sulfonamido)benzoate (compound 14) inhibits the effect onWnt reporter with an IC50value of 7.0 microM, significantly reducesc-MYC levels, inhibits HCT116 colon cancer cell growth (IC5020.2 microM), does not violate Lipinski and Veber rules, and showspredicted Caco-2 and MDCK cell permeability Papp>500 nm s-1.Compound 14 seems to have potential for the development ofnew anticancer therapies.
Sulfonamide inhibitors of beta-catenin signaling as anticancer agents with different output on c-Myc / Di Magno, Laura; Di Pastena, Fiorella; Puxeddu, Michela; La Regina, Giuseppe; Coluccia, Antonio; Ciogli, Alessia; Manetto, Simone; Maroder, Marella; Canettieri, Gianluca; Silvestri, Romano; Nalli, Marianna. - In: CHEMMEDCHEM. - ISSN 1860-7179. - 15(2020), pp. 2264-2268.
Titolo: | Sulfonamide inhibitors of beta-catenin signaling as anticancer agents with different output on c-Myc | |
Autori: | NALLI, Marianna (Corresponding author) | |
Data di pubblicazione: | 2020 | |
Rivista: | ||
Citazione: | Sulfonamide inhibitors of beta-catenin signaling as anticancer agents with different output on c-Myc / Di Magno, Laura; Di Pastena, Fiorella; Puxeddu, Michela; La Regina, Giuseppe; Coluccia, Antonio; Ciogli, Alessia; Manetto, Simone; Maroder, Marella; Canettieri, Gianluca; Silvestri, Romano; Nalli, Marianna. - In: CHEMMEDCHEM. - ISSN 1860-7179. - 15(2020), pp. 2264-2268. | |
Handle: | http://hdl.handle.net/11573/1451071 | |
Appartiene alla tipologia: | 01a Articolo in rivista |
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