Literature DB >> 25666823

Synthesis and SAR study of potent and selective PI3Kδ inhibitors.

Minna Bui1, Xiaolin Hao1, Youngsook Shin1, Mario Cardozo1, Xiao He1, Kirk Henne2, Julia Suchomel1, John McCarter3, Lawrence R McGee1, Tisha San Miguel4, Julio C Medina1, Deanna Mohn4, Thuy Tran2, Sharon Wannberg4, Jamie Wong2, Simon Wong2, Leeanne Zalameda4, Daniela Metz4, Timothy D Cushing1.   

Abstract

2,3,4-Substituted quinolines such as (10a) were found to be potent inhibitors of PI3Kδ in both biochemical and cellular assays with good selectivity over three other class I PI3K isoforms. Some of those analogs showed favorable pharmacokinetic properties.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Autoimmune disorders; Inflammation; PI3Kδ; Reversed quinolines

Mesh:

Substances:

Year:  2015        PMID: 25666823     DOI: 10.1016/j.bmcl.2015.01.001

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


  3 in total

Review 1.  A concise review on hPXR ligand-recognizing residues and structure-based strategies to alleviate hPXR transactivation risk.

Authors:  Tao Liu; James P Beck; Junliang Hao
Journal:  RSC Med Chem       Date:  2022-01-19

2.  Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.

Authors:  Klemens Hoegenauer; Nicolas Soldermann; Frédéric Stauffer; Pascal Furet; Nadege Graveleau; Alexander B Smith; Christina Hebach; Gregory J Hollingworth; Ian Lewis; Sascha Gutmann; Gabriele Rummel; Mark Knapp; Romain M Wolf; Joachim Blanz; Roland Feifel; Christoph Burkhart; Frédéric Zécri
Journal:  ACS Med Chem Lett       Date:  2016-06-02       Impact factor: 4.345

3.  On the hydrolysis of diethyl 2-(perfluorophenyl)malonate.

Authors:  Ilya V Taydakov; Mikhail A Kiskin
Journal:  Beilstein J Org Chem       Date:  2020-07-28       Impact factor: 2.883

  3 in total

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