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Lounsbury N, Mateo G, Jones B, Papaiahgari S, Thimmulappa RK, Teijaro C, Gordon J, Korzekwa K, Ye M, Allaway G, Abou-Gharbia M, Biswal S, Childers W
Heterocyclic chalcone activators of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) with improved in vivo efficacy
Bioorganic and Medicinal Chemistry (2015) 23:5352-9.
Nrf2 activators represent a good drug target for designing agents to treat diseases associated with oxidative stress. Building upon previous work, we designed and prepared a series of heterocyclic chalcone-based Nrf2 activators with reduced lipophilicity and, in some cases, greater in vitro potency compared to the respective carbocyclic scaffold. These changes resulted in enhanced oral bioavailability and a superior pharmacodynamic effect in vivo.
Publication Date: 2015-09-01.
Last updated on Saturday, August 22, 2020