52078-12-3Relevant academic research and scientific papers
N-Aryl benzenesulfonamide inhibitors of [3H]-thymidine incorporation and β-catenin signaling in human hepatocyte-derived Huh-7 carcinoma cells
Kril, Liliia M.,Vilchez, Valery,Jiang, Jieyun,Turcios, Lilia,Chen, Changguo,Sviripa, Vitaliy M.,Zhang, Wen,Liu, Chunming,Spear, Brett,Watt, David S.,Gedaly, Roberto
, p. 3897 - 3899 (2015)
Abstract Structure-activity relationships (SAR) in 2,5-dichloro-N-(2-methyl-4-nitrophenyl)benzenesulfonamide (FH535) were examined as part of a program to identify agents that inhibit the Wnt/β-catenin signaling pathway that is frequently upregulated in hepatocellular carcinoma (HCC). FH535 was reported as an inhibitor of both β-catenin in the Wnt signaling pathway and the peroxisome proliferator-activated receptor (PPAR). A β-catenin/T-cell factor (TCF)/Lymphoid-enhancer factor (LEF)-dependent assay (i.e., luciferase-based TOPFlash assay) as well as a [3H]-thymidine incorporation assay were used to explore SAR modifications of FH535. Although replacing the 2,5-dichlorophenylsulfonyl substituent in FH535 with a 2,6-dihalogenation pattern generally produced more biologically active analogs than FH535, other SAR modifications led only to FH535 analogs with comparable or slightly improved activity in these two assays. The absence of a clear SAR pattern in activity suggested a multiplicity of target effectors for N-aryl benzenesulfonamides.
N-ARYL BENZENESULFONAMIDES FOR USE IN TREATING CANCERS, BACTERIAL DISEASES, METABOLIC DISEASES, AND TRAUMATIC BRAIN INJURY
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Paragraph 0105, (2020/08/28)
Provided herein are methods for treating a disease, such as cancer, the methods including administering one or more N-aryl benezenesulfonamides or analogs thereof to a subject in need thereof.
An Underlying Mechanism of Dual Wnt Inhibition and AMPK Activation: Mitochondrial Uncouplers Masquerading as Wnt Inhibitors
Zhang, Wen,Sviripa, Vitaliy M.,Kril, Liliia M.,Yu, Tianxin,Xie, Yanqi,Hubbard, W. Brad,Sullivan, Patrick G.,Chen, Xi,Zhan, Chang-Guo,Yang-Hartwich, Yang,Evers, B. Mark,Spear, Brett T.,Gedaly, Roberto,Watt, David S.,Liu, Chunming
, p. 11348 - 11358 (2020/01/02)
The importance of upregulated Wnt signaling in colorectal cancers led to efforts to develop inhibitors that target β-catenin in this pathway. We now report that several "Wnt inhibitors" that allegedly target β-catenin actually function as mitochondrial pr
