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 - Lymphocytes B, Autoimmunité et Immunothérapies
4 CalciScreen Platform
5 LCBOSN - Laboratoire de Chimie Bioorganique et des Substances Naturelles
6 ScanMAT - Synthèse Caractérisation Analyse de la Matière

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

Domains: Chemical Sciences

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, 2018, 19 (3), ⟨10.3390/ijms19030856⟩. ⟨hal-01744289⟩