Figure 3.
Design of hybrid photoswitchable RORγ ligands using para‐(ethylsulfonyl) phenylacetamide, a common polar motif for inverse RORγ agonists. a–f) Bistable hybrids MROR 6–9: a–b) design; c) syntheses; d) representative UV/Vis spectra and reversible E Z photoswitching (365/450 nm) (Figure S2bd); e–f) MROR 6–9 have good light‐dependency of cellular RORγ inhibition and high Z‐potency (Figure S3bc). g–k) Fast‐relaxing red‐shifted MROR 10–13 (based on MROR 6–7): g) synthesis; h–i) representative UV/Vis spectra and thermal Z→E isomerisation (Figure S2ce); j–k) light‐dependent cellular RORγ inhibition (Figure S3d). (e, f, j, k: data are mean±S.E.M. from at least 3 independent experiments each with 2 technical replicates). Higher‐resolution Figure given as Figure S8.