Aza-retinoids as novel retinoid X receptor-specific agonists |
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| Authors: | Farmer Luc J Marron Kristen S Canan Koch Stacie S Hwang C K Kallel E Adam Zhi Lin Nadzan Alex M Robertson Dave W Bennani Youssef L |
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| Affiliation: | Ligand Pharmaceuticals Inc., 10255 Science Center Drive, San Diego, CA 92121, USA. luc_farmer@vrtx.com |
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| Abstract: | A new structurally simple series of potent lipophilic aza-retinoids RXR agonists has been developed. SAR studies for the N-alkyl-azadienoic acids described here demonstrate that the RXR activity profile is sensitive to the N-alkyl chain length. Further, we have expanded the work to include azadienoic acids, which exhibited many accessible conformations leading to a better understanding of the SAR around the series. |
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