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

Camille D Dago; Paul Le Maux; Thierry Roisnel; Christophe Brigaudeau; Yves-Alain Békro; Olivier Mignen; Jean-Pierre Bazureau

doi:10.3390/ijms19030856

Journal articles

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

Camille D Dago ^{1, 2} Paul Le Maux ¹ Thierry Roisnel ¹ Christophe Brigaudeau ^{3, 4} Yves-Alain Békro ⁵ Olivier Mignen ^{3, 4, *} Jean-Pierre Bazureau ^{1, 6, *}

* Corresponding author

1 ISCR - Institut des Sciences Chimiques de Rennes

2 LCBOSN - Laboratoire de Chimie Bioorganique et des Substances Naturelles

3 LBAI - Lymphocyte B et Auto-immunité

4 CalciScreen Platform

5 LCBOSN - Laboratoire de Chimie Bioorganique et des Substances Naturelles

6 ScanMAT - Synthèse Caractérisation Analyse de la Matière

Abstract : From a series of (1, 1)-1[β-(phenylalkoxy)-(phenetyl)]-1-pyrazolium hydrochloride as new analogues of SKF-96365, one has an interesting effect for endoplasmic reticulum (ER) Carelease and store-operated Caentry (SOCE) (IC25 μM) on the PLP-B lymphocyte cell line. A successful resolution of (±) 1-phenyl-2-(1-pyrazol-1-yl)ethan-1-ol has been developed by using the method of "half-concentration" in the presence of (+)-(1)- or (-)-(1)-CSA.

Keywords : half-quantities pyrazole resolution analogues B lymphocyte cell Ca2+ signalling SKF-96365 SOCE SOCE inhibitor

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Journal articles

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Chemical Sciences

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

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

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