- Preliminary Structure-Activity Relationship (SAR) of a Novel Series of Pyrazole SKF-96365 Analogues as Potential Store-Operated Calcium Entry (SOCE) Inhibitors.
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 (2018-03-15)
Camille D Dago, Paul Le Maux, Thierry Roisnel, Christophe Brigaudeau, Yves-Alain Bekro, Olivier Mignen, Jean-Pierre Bazureau
PMID29538341
ABSTRACT
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) Ca2+ release and store-operated Ca2+ entry (SOCE) (IC50 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.
MATERIALS