X receptor (PXR) plays roles in detoxification and other
physiological processes. PXR activation may enhance drug metabolism
(leading to adverse drug reactions) or inhibit inflammation. Therefore,
PXR agonists, antagonists, and inverse agonists may serve as research
tools and drug candidates. However, a specific PXR modulator with
an associated structure–activity relationship is lacking. Based
on the scaffold of specific human PXR (hPXR) antagonist SPA70 (10), we developed 81 SPA70 analogs and evaluat… Show more
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