| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10596070 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
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. 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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
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,