NDLI: Identification of potent RORβ modulators: Scaffold variation

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Identification of potent RORβ modulators: Scaffold variation

Content Provider	Scilit
Author	Doebelin, Christelle Patouret, Rémi Garcia-Ordonez, Ruben D. Chang, Mi Ra Dharmarajan, Venkatasubramanian Novick, Scott Ciesla, Anthony Campbell, Sean Solt, Laura A. Griffin, Patrick R. Kamenecka, Theodore M.
Copyright Year	2018
Description	Journal: Bioorganic & medicinal chemistry letters We sought to develop RORβ-selective probe molecules in order to investigate the function of the receptor in vitro and in vivo and its role in the pathophysiology of disease. To accomplish this, we modified a potent dual RORβ/RORγ inverse agonist from the primary literature with the goal of improving selectivity for RORβ vs RORγ. Truncation of the Western portion of the molecule ablated activity at RORγ and led to a potent series of RORβ modulators. Continued exploration of this series investigated alternate replacement cores for the aminothiazole ring. Numerous suitable replacements were found during the course of our SAR investigations and are reported herein.
Related Links	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6238650/pdf
Ending Page	3215
Page Count	6
Starting Page	3210
ISSN	0960894X
DOI	10.1016/j.bmcl.2018.08.017
Journal	Bioorganic & medicinal chemistry letters
Issue Number	19
Volume Number	28
Language	English
Publisher	Elsevier BV
Publisher Date	2018-10-01
Access Restriction	Open
Subject Keyword	Journal: Bioorganic & medicinal chemistry letters Medicinal Chemistry
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Drug Discovery Biochemistry Molecular Biology Clinical Biochemistry Molecular Medicine Pharmaceutical Science

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