title: Biological Evaluationin Vitroandin Silicoof Azetidin-2-one Derivatives as Potential Anticancer Agents.
abstract: Potential anticancer activity of 16 azetidin-2-one derivatives was evaluated showing that compound6[N-(p-methoxy-phenyl)-2-(p-methyl-phenyl)-3-phenoxy-azetidin-2-one] presented cytotoxic activity in SiHa cells and B16F10 cells. The caspase-3 assay in B16F10 cells displayed that azetidin-2-one derivatives induce apoptosis. Microarray and molecular analysis showed that compound6was involved on specific gene overexpression of cytoskeleton regulation and apoptosis due to the inhibition of some cell cycle genes. From the 16 derivatives, compound6showed the highest selectivity to neoplastic cells, it was an inducer of apoptosis, and according to anin silicoanalysis of chemical interactions with colchicine binding site of human α/β-tubulin, the mechanism of action could be a molecular interaction involving the amino acids outlining such binding site.
authors.affiliation: Universidad Autonoma de Nuevo Leon , Facultad de Ciencias Químicas, Monterrey, México.
authors.forename: Fabián E
authors.initials: FE
authors.lastname: Olazaran
authors.affiliation: Centro de Biotecnología Genómica, Instituto Politécnico Nacional , Reynosa, México.
authors.forename: Gildardo
authors.initials: G
authors.lastname: Rivera
authors.affiliation: Centro de Biotecnología Genómica, Instituto Politécnico Nacional , Reynosa, México.
authors.forename: Alondra M
authors.initials: AM
authors.lastname: Pérez-Vázquez
authors.affiliation: Centro de Biotecnología Genómica, Instituto Politécnico Nacional , Reynosa, México.
authors.forename: Cynthia M
authors.initials: CM
authors.lastname: Morales-Reyes
authors.affiliation: Red de Estudios Moleculares Avanzados, Instituto de Ecología , A.C., Xalapa Enríquez, México.
authors.forename: Aldo
authors.initials: A
authors.lastname: Segura-Cabrera
authors.affiliation: Universidad Autonoma de Nuevo Leon , Facultad de Ciencias Químicas, Monterrey, México.
authors.forename: Isaías
authors.initials: I
authors.lastname: Balderas-Rentería
keywords: Azetidin-2-one; anticancer; apoptosis; docking; microarray; β-tubulin