bardoxolone-methyl and sulforaphane

bardoxolone-methyl has been researched along with sulforaphane* in 1 studies

Other Studies

1 other study(ies) available for bardoxolone-methyl and sulforaphane

Article	Year
Discovery of a crystalline sulforaphane analog with good solid-state stability and engagement of the Nrf2 pathway in vitro and in vivo. Bioorganic & medicinal chemistry, 2019, 02-15, Volume: 27, Issue:4 The antioxidant natural product sulforaphane (SFN) is an oil with poor aqueous and thermal stability. Recent work with SFN has sought to optimize methods of formulation for oral and topical administration. Herein we report the design of new analogs of SFN with the goal of improving stability and drug-like properties. Lead compounds were selected based on potency in a cellular screen and physicochemical properties. Among these, 12 had good aqueous solubility, permeability and long-term solid-state stability at 23 °C. Compound 12 also displayed comparable or better efficacy in cellular assays relative to SFN and had in vivo activity in a mouse cigarette smoke challenge model of acute oxidative stress. Topics: Animals; Antioxidants; Cell Line; Cyclobutanes; Drug Discovery; Gene Expression; Heme Oxygenase-1; Humans; Isothiocyanates; Kelch-Like ECH-Associated Protein 1; Mice, Inbred C57BL; Molecular Structure; NF-E2-Related Factor 2; Oxidative Stress; Rats; Signal Transduction; Solubility; Structure-Activity Relationship; Sulfoxides; Thiocarbamates	2019

Article

Year

Discovery of a crystalline sulforaphane analog with good solid-state stability and engagement of the Nrf2 pathway in vitro and in vivo.

Bioorganic & medicinal chemistry, 2019, 02-15, Volume: 27, Issue:4

The antioxidant natural product sulforaphane (SFN) is an oil with poor aqueous and thermal stability. Recent work with SFN has sought to optimize methods of formulation for oral and topical administration. Herein we report the design of new analogs of SFN with the goal of improving stability and drug-like properties. Lead compounds were selected based on potency in a cellular screen and physicochemical properties. Among these, 12 had good aqueous solubility, permeability and long-term solid-state stability at 23 °C. Compound 12 also displayed comparable or better efficacy in cellular assays relative to SFN and had in vivo activity in a mouse cigarette smoke challenge model of acute oxidative stress.

Topics: Animals; Antioxidants; Cell Line; Cyclobutanes; Drug Discovery; Gene Expression; Heme Oxygenase-1; Humans; Isothiocyanates; Kelch-Like ECH-Associated Protein 1; Mice, Inbred C57BL; Molecular Structure; NF-E2-Related Factor 2; Oxidative Stress; Rats; Signal Transduction; Solubility; Structure-Activity Relationship; Sulfoxides; Thiocarbamates

2019