16855-41-7Relevant academic research and scientific papers
Synthesis and Evaluation of Noncovalent Naphthalene-Based KEAP1-NRF2 Inhibitors
David, Brian P.,Jain, Atul D.,Lazzara, Phillip R.,Maldonado, Amanda C.,Moore, Terry W.,Ratia, Kiira M.,Richardson, Benjamin,Siddiqui, Zamia,Skowron, Kornelia J.
, p. 521 - 527 (2020)
The oxidative stress response, gated by the protein-protein interaction of KEAP1 and NRF2, has garnered significant interest in the past decade. Misregulation in this pathway has been implicated in disease states such as multiple sclerosis, rheumatoid arthritis, and diabetic chronic wounds. Many of the known activators of NRF2 are electrophilic in nature and may operate through several biological pathways rather than solely through the activation of the oxidative stress response. Recently, our lab has reported a nonelectrophilic, monoacidic, naphthalene-based NRF2 activator which exhibited good potency in vitro. Herein, we report a detailed structure-activity relationship of naphthalene-based NRF2 activators, an X-ray crystal structure of our monoacidic KEAP1 inhibitor, and identification of an underexplored area of the NRF2 binding pocket of KEAP1.
1,4-SUBSTITUTED ISOQUINOLINE INHIBITORS OF KEAP1/NRF2 PROTEIN-PROTEIN INTERACTION
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Paragraph 00102, (2019/10/29)
Disclosed herein are compounds that can act as inhibitors of the Kelch-like ECH- associated protein 1/nuclear factor (erythroid-derived 2)-like 2 ("KEAP1/NRF2") protein- protein interaction, and methods of using the compounds to treat and prevent diseases and disorders, such as COPD, multiple sclerosis, and diabetes, and in the promotion of wound healing. The compounds described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: formula (I), wherein the substituents are as described.
Preparation of a series of substituted fluoromethylnaphthalenes
Dixon, Elisabeth A.,Fischer, Alfred,Robinson, Frank P.
, p. 2629 - 2641 (2007/10/02)
A series of 22 3- and 4-substituted 1-fluoromethylnaphthalenes have been synthesized.Details of practical procedures for the preparation of all intermediates are described, and physical properties for all of the substituted naphthalenes synthesized, and spectral parameters for 51 previously unknown compounds, are given.
