| publication name | Small molecule amides as potent ROR-γ selective modulators |
|---|---|
| Authors | Pasha M. Khan, Bahaa El-Dien M. El-Gendy, Naresh Kumar, Ruben Garcia-Ordonez, Li Lin, Claudia H. Ruiz, Michael D. Cameron, Patrick R. Griffin, Theodore M. Kamenecka |
| year | 2013 |
| keywords | |
| journal | |
| volume | Not Available |
| issue | Not Available |
| pages | Not Available |
| publisher | Not Available |
| Local/International | International |
| Paper Link | http://www.sciencedirect.com/science/article/pii/S0960894X12014680 |
| Full paper | download |
| Supplementary materials | Not Available |
Abstract
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.