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

Potential anticancer activity of 16 azetidin-2-one derivatives was evaluated showing that compound [-(-methoxy-phenyl)-2-(-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 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 showed the highest selectivity to neoplastic cells, it was an inducer of apoptosis, and according to an analysis 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.