Staff Members - Benha University
Small molecule amides as potent ROR-γ selective modulators
• 2013
Publication Information
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
Keywords
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Journal
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Publisher
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Volume
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Issue
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Pages
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publication.type
International
Paper Link
Open Link
Supplementary Materials
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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.