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
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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Camille D Dago, Paul Le Maux, Thierry Roisnel, Christophe Brigaudeau, Yves-Alain Békro, et al.. Preliminary Structure-Activity Relationship (SAR) of a Novel Series of Pyrazole SKF-96365 Analogues as Potential Store-Operated Calcium Entry (SOCE) Inhibitors. International Journal of Molecular Sciences, MDPI, 2018, 19 (3), ⟨10.3390/ijms19030856⟩. ⟨hal-01744289⟩

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