Literature DB >> 22560469

Synthesis and SAR of tetrahydroisoquinolines as Rev-erbα agonists.

Romain Noel1, Xinyi Song, Youseung Shin, Subhashis Banerjee, Douglas Kojetin, Li Lin, Claudia H Ruiz, Michael D Cameron, Thomas P Burris, Theodore M Kamenecka.   

Abstract

The design and synthesis of a novel series of Rev-erbα agonists is described. The development and optimization of the tetrahydroisoquinoline series was carried out from an earlier acyclic series of Rev-erbα agonists. Through the optimization of the scaffold 1, several potent compounds with good in vivo profiles were discovered.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID： 22560469      PMCID： PMC3488456          DOI： 10.1016/j.bmcl.2012.04.023

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  14 in total

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Journal:  Chem Biol       Date:  2012-01-27

2.  Rev-erbalpha, a heme sensor that coordinates metabolic and circadian pathways.

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5.  Cross-talk among ROR alpha 1 and the Rev-erb family of orphan nuclear receptors.

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6.  A new orphan member of the nuclear hormone receptor superfamily closely related to Rev-Erb.

Authors:  B Dumas; H P Harding; H S Choi; K A Lehmann; M Chung; M A Lazar; D D Moore
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Journal:  Adv Drug Deliv Rev       Date:  2010-07-22       Impact factor: 15.470

Review 9.  Nuclear hormone receptors for heme: REV-ERBalpha and REV-ERBbeta are ligand-regulated components of the mammalian clock.

Authors:  Thomas P Burris
Journal:  Mol Endocrinol       Date:  2008-01-24

10.  Identification of heme as the ligand for the orphan nuclear receptors REV-ERBalpha and REV-ERBbeta.

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Journal:  Nat Struct Mol Biol       Date:  2007-11-25       Impact factor: 15.369
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Authors:  Edward Ofori; Xue Y Zhu; Jagan R Etukala; Barbara A Bricker; Seth Y Ablordeppey
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7.  REV-ERBα Regulates TH17 Cell Development and Autoimmunity.

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  8 in total

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