Oxazolidinone derivatives: Cytoxazone–Linezolid hybrids induces apoptosis and senescence in DU145 prostate cancer cells

• A novel series of oxazolidinones have been synthesized.
• The series of compounds were evaluated for their anticancer potential.
• Couple of compounds exhibited significant inhibitory activity against cancer cells.
• Compound 17 induces cellular senescence and apoptosis of DU145 cells.
• This study finds oxazolidinones as novel anticancer agents.

In this study, we report the synthesis of novel oxazolidinone derivatives derived from linezolid 3 having p-methoxyphenyl group at C-4 position. In vitro evaluation for their anticancer activity toward cultured A549, DU145, HELA, and MCF7 were carried out. The series of compounds prepared displayed wide range of cytotoxicity in MTT assays (10–70 μM) across the cell lines tested. Of the all tested compounds 16 and 17 displayed good anticancer potential against A549 (lung) and DU145 (prostate) cancer cells. Further, to determine their anticancer potential, in the present study we have assessed effect of 17 on DU145 cells growth in in vitro assays. The results clearly demonstrated that the exposure of DU145 cells to 17 inhibits cell proliferation and induces apoptosis by activation of caspase-3 and -9. Long term exposure of DU145 cells to 17 induced cellular senescence confirmed by senescence marker β-galactosidase staining of cells on post exposure to 17. The results from this current report support that the oxazolidinone derivatives with ethyl and acryl substitutions showed promising anticancer activity which will be helpful to develop further novel anticancer agents with better therapeutic potential.

A novel series of oxazolidinones having p-methoxy phenyl group at C-4 position have been synthesized. Compound 17 induces cellular senescence and apoptosis in DU145 prostate cancer cells.Figure optionsDownload as PowerPoint slide