1426148-73-3Relevant articles and documents
Small molecule amides as potent ROR-γ selective modulators
Khan, Pasha M.,El-Gendy, Bahaa El-Dien M.,Kumar, Naresh,Garcia-Ordonez, Ruben,Lin, Li,Ruiz, Claudia H.,Cameron, Michael D.,Griffin, Patrick R.,Kamenecka, Theodore M.
, p. 532 - 536 (2013/02/25)
The structure-activity relationship study of a diphenylpropanamide series of ROR-γ selective modulators is reported. Compounds were screened using chimeric receptor Gal4 DNA-binding domain (DBD)-NR ligand binding domain cotransfection assay in a two-step format. Three different regions of the scaffold were modified to assess the effects on repression of ROR-γ transcriptional activity and potency. The lead compound 1 exhibits modest mouse pharmacokinetics and an acceptable in vitro profile which makes it a suitable in vivo probe to interrogate the functions of ROR-γ in animal models of disease.
