1417802-79-9Relevant academic research and scientific papers
A-ring modification of SCH 900229 and related chromene sulfone γ-secretase inhibitors
Wu, Wen-Lian,Sasikumar, Thavalakulamgara K.,Domalski, Martin S.,Qiang, Li,Burnett, Duane A.,Clader, John,Greenlee, William J.,Chan, Tze-Ming,Lee, Julie,Zhang, Lili
, p. 850 - 853 (2013/02/25)
Attempts to block metabolism by incorporating a 9-fluoro substituent at the A-ring of compound 1 (SCH 900229) using electrophilic Selectfluor led to an unexpected oxidation of the A-ring to give difluoroquinone analog 1a. Oxidation of other related chromene γ-secretase inhibitors 2-8 resulted in similar difluoroquinone analogs 2a-8a, respectively. These quinone products exhibited comparable in vitro potency in a γ-scretase membrane assay, but were several fold less potent in a cell-based assay in lowering Aβ40-42, compared to their parent compounds.
