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Biological Evaluation in Vitro and in Silico of Azetidin-2-one Derivatives as Potential Anticancer Agents.

ABSTRACT: Potential anticancer activity of 16 azetidin-2-one derivatives was evaluated showing that compound 6 [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 compound 6 was involved on specific gene overexpression of cytoskeleton regulation and apoptosis due to the inhibition of some cell cycle genes. From the 16 derivatives, compound 6 showed the highest selectivity to neoplastic cells, it was an inducer of apoptosis, and according to an in silico analysis of chemical interactions with colchicine binding site of human ?/?-tubulin, the mechanism of action could be a molecular interaction involving the amino acids outlining such binding site.

SUBMITTER: Olazaran FE

PROVIDER: S-EPMC5238468 | biostudies-literature | 2017 Jan

REPOSITORIES: biostudies-literature

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Biological Evaluation in Vitro and in Silico of Azetidin-2-one Derivatives as Potential Anticancer Agents.

Olazaran Fabián E FE Rivera Gildardo G Pérez-Vázquez Alondra M AM Morales-Reyes Cynthia M CM Segura-Cabrera Aldo A Balderas-Rentería Isaías I

ACS medicinal chemistry letters 20161110 1

Potential anticancer activity of 16 azetidin-2-one derivatives was evaluated showing that compound 6 [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 compound 6 was involved on specific gene overexpression of cytoskeleton regulation and apopto ...[more]

PMID: 28105271

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Dataset Information

Biological Evaluation in Vitro and in Silico of Azetidin-2-one Derivatives as Potential Anticancer Agents.

Publications

Biological Evaluation <i>in Vitro</i> and <i>in Silico</i> of Azetidin-2-one Derivatives as Potential Anticancer Agents.

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