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

Int J Mol Sci. 2018 Mar 14;19(3):856. doi: 10.3390/ijms19030856.

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.

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

MeSH terms

  • Calcium Channel Blockers / chemical synthesis*
  • Calcium Channel Blockers / chemistry
  • Calcium Channel Blockers / pharmacology
  • Calcium Signaling / drug effects*
  • Cell Line, Tumor
  • Humans
  • Imidazoles / chemistry*
  • Imidazoles / pharmacology
  • Quantitative Structure-Activity Relationship*

Substances

  • Calcium Channel Blockers
  • Imidazoles
  • 1-(2-(3-(4-methoxyphenyl)propoxy)-4-methoxyphenylethyl)-1H-imidazole