Structural modification of C2-substituents on 1,4-bis(arylsulfonamido)benzene or naphthalene-N,N'-diacetic acid derivatives as potent inhibitors of the Keap1-Nrf2 protein-protein interaction.

The Keap1-Nrf2-ARE signaling pathway is an attractive therapeutic target for the prevention and treatment of oxidative stress-associated diseases by activating the cellular expression of cytoprotective enzymes and proteins. Small molecule inhibitors can directly disrupt the Keap1-Nrf2 protein-protein interaction (PPI), resulting in elevated levels of Nrf2 protein and subsequent stimulation of related antioxidant responses. Previously, we found that 1,4-bis(arylsulfonamido)benzene or naphthalene-N,N'-diacetic acid derivatives with an ether type C2-substituent on the benzene or naphthalene core exhibited potent inhibitory activities with IC

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Déclaration de conflit d'intérêts

Declaration of competing interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Longqin Hu reports financial support was provided by National Institutes of Health. Longqin Hu reports financial support was provided by Rutgers The State University of New Jersey. Longqin Hu reports a relationship with Rutgers The State University of New Jersey that includes: employment. Michael P. Verzi reports a relationship with Rutgers The State University of New Jersey that includes: employment. Sumi Lee reports a relationship with Rutgers The State University of New Jersey that includes: employment. Ahmed R. Ali reports a relationship with Rutgers The State University of New Jersey that includes: employment. Dhulfiqar Ali Abed reports a relationship with Rutgers The State University of New Jersey that includes: employment. Mai-Uyen Nguyen reports a relationship with Rutgers The State University of New Jersey that includes: employment. Longqin Hu has patent #Small Molecule Direct Inhibitors of Keap1-Nrf2 Protein-Protein Interaction pending to Rutgers The State University of New Jersey. Dhulfiqar Ali Abed has patent #Small Molecule Direct Inhibitors of Keap1-Nrf2 Protein-Protein Interaction pending to Rutgers The State University of New Jersey. Ahmed R. Ali has patent #Small Molecule Direct Inhibitors of Keap1-Nrf2 Protein-Protein Interaction pending to Rutgers The State University of New Jersey.