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Dr. Bahaa El-Dien M. El-Gendy :: Publications: |
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| Title: | Small molecule amides as potent ROR-γ selective modulators
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| 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: | Not Available |
| Journal: | Not Available |
| Volume: | Not Available |
| Issue: | Not Available |
| Pages: | Not Available |
| Publisher: | Not Available |
| Local/International: | International |
| Paper Link: | |
| Full paper | Not Available |
| 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. |
