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Design and synthesis of a potent, highly selective, orally bioavailable, retinoic acid receptor alpha agonist
A ligand-based virtual screening exercise examining likely bioactive conformations of AM 580 (2) and AGN 193836 (3) was used to identify the novel, less lipophilic RARα agonist 4-(3,5-dichloro-4-ethoxybenzamido)benzoic acid 5, which has good selectivity over the RARβ, and RARγ receptors. Analysis of...
Autores principales: | Clarke, Earl, Jarvis, Christopher I., Goncalves, Maria B., Kalindjian, S. Barret, Adams, David R., Brown, Jane T., Shiers, Jason J., Taddei, David M.A., Ravier, Elodie, Barlow, Stephanie, Miller, Iain, Smith, Vanessa, Borthwick, Alan D., Corcoran, Jonathan P.T. |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier Science
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5823845/ https://www.ncbi.nlm.nih.gov/pubmed/29288071 http://dx.doi.org/10.1016/j.bmc.2017.12.015 |
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