| Literature DB >> 23232056 |
Pasha M Khan1, 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.
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.Entities:
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Year: 2012 PMID： 23232056 PMCID： PMC3534870 DOI： 10.1016/j.bmcl.2012.11.025
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823