Preliminary Structure-Activity Relationship (SAR) of a Novel Series of Pyrazole SKF-96365 Analogues as Potential Store-Operated Calcium Entry (SOCE) Inhibitors

From a series of (1R, 1S)-1[β-(phenylalkoxy)-(phenetyl)]-1H-pyrazolium hydrochloride as new analogues of SKF-96365, one has an interesting effect for endoplasmic reticulum (ER) Ca(2+) release and store-operated Ca(2+) entry (SOCE) (IC(50) 25 μM) on the PLP-B lymphocyte cell line. A successful resolu...

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Autores principales: Dago, Camille D., Maux, Paul Le, Roisnel, Thierry, Brigaudeau, Christophe, Bekro, Yves-Alain, Mignen, Olivier, Bazureau, Jean-Pierre
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5877717/
https://www.ncbi.nlm.nih.gov/pubmed/29538341
http://dx.doi.org/10.3390/ijms19030856
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author Dago, Camille D.
Maux, Paul Le
Roisnel, Thierry
Brigaudeau, Christophe
Bekro, Yves-Alain
Mignen, Olivier
Bazureau, Jean-Pierre
author_facet Dago, Camille D.
Maux, Paul Le
Roisnel, Thierry
Brigaudeau, Christophe
Bekro, Yves-Alain
Mignen, Olivier
Bazureau, Jean-Pierre
author_sort Dago, Camille D.
collection PubMed
description From a series of (1R, 1S)-1[β-(phenylalkoxy)-(phenetyl)]-1H-pyrazolium hydrochloride as new analogues of SKF-96365, one has an interesting effect for endoplasmic reticulum (ER) Ca(2+) release and store-operated Ca(2+) entry (SOCE) (IC(50) 25 μM) on the PLP-B lymphocyte cell line. A successful resolution of (±) 1-phenyl-2-(1H-pyrazol-1-yl)ethan-1-ol has been developed by using the method of “half-concentration” in the presence of (+)-(1S)- or (−)-(1R)-CSA.
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spelling pubmed-58777172018-04-09 Preliminary Structure-Activity Relationship (SAR) of a Novel Series of Pyrazole SKF-96365 Analogues as Potential Store-Operated Calcium Entry (SOCE) Inhibitors Dago, Camille D. Maux, Paul Le Roisnel, Thierry Brigaudeau, Christophe Bekro, Yves-Alain Mignen, Olivier Bazureau, Jean-Pierre Int J Mol Sci Article From a series of (1R, 1S)-1[β-(phenylalkoxy)-(phenetyl)]-1H-pyrazolium hydrochloride as new analogues of SKF-96365, one has an interesting effect for endoplasmic reticulum (ER) Ca(2+) release and store-operated Ca(2+) entry (SOCE) (IC(50) 25 μM) on the PLP-B lymphocyte cell line. A successful resolution of (±) 1-phenyl-2-(1H-pyrazol-1-yl)ethan-1-ol has been developed by using the method of “half-concentration” in the presence of (+)-(1S)- or (−)-(1R)-CSA. MDPI 2018-03-14 /pmc/articles/PMC5877717/ /pubmed/29538341 http://dx.doi.org/10.3390/ijms19030856 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Dago, Camille D.
Maux, Paul Le
Roisnel, Thierry
Brigaudeau, Christophe
Bekro, Yves-Alain
Mignen, Olivier
Bazureau, Jean-Pierre
Preliminary Structure-Activity Relationship (SAR) of a Novel Series of Pyrazole SKF-96365 Analogues as Potential Store-Operated Calcium Entry (SOCE) Inhibitors
title Preliminary Structure-Activity Relationship (SAR) of a Novel Series of Pyrazole SKF-96365 Analogues as Potential Store-Operated Calcium Entry (SOCE) Inhibitors
title_full Preliminary Structure-Activity Relationship (SAR) of a Novel Series of Pyrazole SKF-96365 Analogues as Potential Store-Operated Calcium Entry (SOCE) Inhibitors
title_fullStr Preliminary Structure-Activity Relationship (SAR) of a Novel Series of Pyrazole SKF-96365 Analogues as Potential Store-Operated Calcium Entry (SOCE) Inhibitors
title_full_unstemmed Preliminary Structure-Activity Relationship (SAR) of a Novel Series of Pyrazole SKF-96365 Analogues as Potential Store-Operated Calcium Entry (SOCE) Inhibitors
title_short Preliminary Structure-Activity Relationship (SAR) of a Novel Series of Pyrazole SKF-96365 Analogues as Potential Store-Operated Calcium Entry (SOCE) Inhibitors
title_sort preliminary structure-activity relationship (sar) of a novel series of pyrazole skf-96365 analogues as potential store-operated calcium entry (soce) inhibitors
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5877717/
https://www.ncbi.nlm.nih.gov/pubmed/29538341
http://dx.doi.org/10.3390/ijms19030856
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