Synthesis and SAR of tetrahydroisoquinolines as Rev-erbα agonists.

Bioorganic & Medicinal Chemistry Letters
Romain NoelTheodore 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.

References

Apr 30, 2010·Endocrinology·Naresh KumarThomas P Burris
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Apr 30, 2011·Future Medicinal Chemistry·Laura A SoltThomas P Burris

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Citations

Mar 1, 2014·Nature Reviews. Drug Discovery·Douglas J Kojetin, Thomas P Burris
Jun 16, 2015·Biochemical Pharmacology·Yongjun WangThomas P Burris
Nov 29, 2016·Journal of Inorganic Biochemistry·Eduardo Henrique Silva SousaMarie-Alda Gilles-Gonzalez
Dec 24, 2014·Nature Communications·Subhashis BanerjeeThomas P Burris
Jun 9, 2020·Journal of Enzyme Inhibition and Medicinal Chemistry·Shenzhen HuangZhijie Li
May 11, 2015·FEBS Letters·Thomas Wallach, Achim Kramer
Aug 3, 2020·Bioorganic & Medicinal Chemistry Letters·Amaia Uriz-HuarteMatthew J Fuchter
Apr 14, 2021·Oncogene·Francesca BattaglinHeinz-Josef Lenz
Jul 13, 2021·Journal of Medicinal Chemistry·Sabine WillemsDaniel Merk
Oct 26, 2016·Bioorganic & Medicinal Chemistry·Edward OforiSeth Y Ablordeppey

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