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...

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Pubblicato in:Bioorg Med Chem
Autori principali: 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.
Natura: Artigo
Lingua:Inglês
Pubblicazione: Elsevier Science 2018
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Article
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC5823845/
https://ncbi.nlm.nih.gov/pubmed/29288071
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmc.2017.12.015
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