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Design, characterization and quantum chemical computations of a novel series of pyrazoles derivatives with potential anti-proinflammatory response

dc.contributor.authorBurboa-Schettino P.
dc.contributor.authorBustos C.
dc.contributor.authorMolins E.
dc.contributor.authorFigueroa X.F.
dc.contributor.authorLlanquinao J.
dc.contributor.authorZarate X.
dc.contributor.authorVallejos G.
dc.contributor.authorDiaz-Uribe C.
dc.contributor.authorVallejo W.
dc.contributor.authorSchott E.
dc.date.accessioned2020-09-02T22:13:35Z
dc.date.available2020-09-02T22:13:35Z
dc.date.issued2020
dc.identifier10.1016/j.arabjc.2020.05.042
dc.identifier.citation13, 8, 6412-6424
dc.identifier.issn18785352
dc.identifier.urihttps://hdl.handle.net/20.500.12728/3801
dc.descriptionThe 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. © 2020 The Author(s)
dc.language.isoen
dc.publisherElsevier B.V.
dc.subjectAnti-proinflammatory
dc.subjectDFT
dc.subjectNCI-60
dc.subjectPlatelet-activating factor
dc.subjectPyrazoles
dc.subjectCell culture
dc.subjectDesign for testability
dc.subjectNuclear magnetic resonance spectroscopy
dc.subjectPhospholipids
dc.subjectBiological actions
dc.subjectCancer cell lines
dc.subjectPlatelet-activating factors
dc.subjectProinflammatory
dc.subjectProinflammatory response
dc.subjectQuantum chemical computations
dc.subjectSynthesis and characterizations
dc.subjectTwo-dimensional NMR
dc.subjectQuantum chemistry
dc.titleDesign, characterization and quantum chemical computations of a novel series of pyrazoles derivatives with potential anti-proinflammatory response
dc.typeArticle


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