Fondo Nacional de Desarrollo Científico y Tecnológico (Chile), Ministerio de Economía, Fomento y Turismo (Chile), Universidad del Atlántico, Burboa-Schettino, Pia, Bustos, Carlos, Molins, Elies, Figueroa, Xavier F., Llanquinao, Jesus, Zarate, Ximena, Vallejos, Gabriel, Diaz Uribe, Carlos, Vallejo, William, Schott, Eduardo, Fondo Nacional de Desarrollo Científico y Tecnológico (Chile), Ministerio de Economía, Fomento y Turismo (Chile), Universidad del Atlántico, Burboa-Schettino, Pia, Bustos, Carlos, Molins, Elies, Figueroa, Xavier F., Llanquinao, Jesus, Zarate, Ximena, Vallejos, Gabriel, Diaz Uribe, Carlos, Vallejo, William, and Schott, Eduardo
The synthesis and characterization of the full family of 11 pyrazoles were performed by means of UV–Vis, FTIR, 1H NMR, 13C NMR, two-dimensional NMR experiments and DFT simulations. As pyrazoles are known for showing diverse biological actions, they were also tested in the NCI-60 cancer cell line panel, showing moderate to good activity against different cell lines. Furthermore, the anti-proinflammatory activity test of a set of pyrazoles of the form (E)-4-((4-bromophenyl)diazenyl)-3,5-dimethyl-1-R-phenyl-1H-pyrazole was performed, this is based on the study of the blockage of the increase in intracellular [Ca2+] observed in response to platelet-activating factor (PAF) treatment of four pyrazoles (i.e. 6, 8, 9 and 10), which successfully displayed [Ca2+] channel inhibition. Therefore, the obtained intracellular [Ca2+] signal results indicate that the pyrazole family characterized in this study, in particular compounds 6 and 10, are potent blockers of the PAF-initiated Ca2+ signaling that mediates the hyperpermeability typically observed during the development of inflammation.