Synthesis and structure-activity relationships of potent retinoid X receptor ligands
| Autor: | Glenn Croston, Susan Jeong, Luc J. Farmer, Rich A. Heyman, Karen S. Flatten, E. Adam Kallel, Alex M. Nadzan, Stacie S. Canan Koch |
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| Rok vydání: | 1997 |
| Předmět: |
Agonist
Chemistry medicine.drug_class Stereochemistry Organic Chemistry Clinical Biochemistry Pharmaceutical Science Retinoid X receptor Biochemistry Chemical synthesis Transactivation chemistry.chemical_compound Drug Discovery medicine Molecular Medicine Moiety Retinoid Receptor Molecular Biology Lead compound |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 7:2393-2398 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(97)00437-x |
| Popis: | A series of potent retinoid X receptor (RXR) selective ligands was designed and prepared. The lead compound 7a showed good binding (K i ; 20–50 nM) and transactivation (EC 50 ; 40–50 nM) to the RXR subfamily of retinoid receptors. More importantly, small variations in the geometry of the cyclopentane ring moiety led to 9 , one of the most potent RXR agonists to date (K i : 3–8 nM; EC 50 : 3–4 nM). |
| Databáze: | OpenAIRE |
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