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Sulfonamide Inhibitors of ß-Catenin Signaling with Different Output on c-MYC as Anticancer Agents.
ChemMedChem ( IF 3.6 ) Pub Date : 2020-09-18 , DOI: 10.1002/cmdc.202000594 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
ChemMedChem ( IF 3.6 ) Pub Date : 2020-09-18 , DOI: 10.1002/cmdc.202000594 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
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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.
中文翻译：
β-连环蛋白信号的磺胺抑制剂在 c-MYC 上具有不同的输出，作为抗癌剂。
Wnt/β-catenin 通路在癌症中经常被发现失调。β-连环蛋白在细胞核中的异常积累导致各种恶性肿瘤的发展。针对这一信号通路的特定药物尚未获批用于临床治疗。在此，我们报告了具有潜在治疗价值的 β-catenin 信号抑制剂作为抗癌剂。Ethyl 4-((4-(trifluoromethyl)phenyl)sulfonamido)benzoate（化合物14）抑制对 Wnt 报告基因的影响，IC 50值为 7.0 μM，显着降低 c-MYC 水平，抑制 HCT116 结肠癌细胞生长（IC 50 20.2 μM)，不违反 Lipinski 和 Veber 规则，并显示预测的 Caco-2 和 MDCK 细胞通透性P app > 500 nm s-1。化合物14似乎具有开发新抗癌疗法的潜力。
更新日期：2020-09-18
中文翻译：
β-连环蛋白信号的磺胺抑制剂在 c-MYC 上具有不同的输出，作为抗癌剂。
Wnt/β-catenin 通路在癌症中经常被发现失调。β-连环蛋白在细胞核中的异常积累导致各种恶性肿瘤的发展。针对这一信号通路的特定药物尚未获批用于临床治疗。在此，我们报告了具有潜在治疗价值的 β-catenin 信号抑制剂作为抗癌剂。Ethyl 4-((4-(trifluoromethyl)phenyl)sulfonamido)benzoate（化合物14）抑制对 Wnt 报告基因的影响，IC 50值为 7.0 μM，显着降低 c-MYC 水平，抑制 HCT116 结肠癌细胞生长（IC 50 20.2 μM)，不违反 Lipinski 和 Veber 规则，并显示预测的 Caco-2 和 MDCK 细胞通透性P app > 500 nm s-1。化合物14似乎具有开发新抗癌疗法的潜力。
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