Abstract

SYNTHESIS AND DESIGN OF A NOVEL SUBSTITUTED MORPHOLINE DERIVATIVES AND EVALUATION FORTHEIR ANTICANCER ACTIVITY

*A. Chitra, J. Revathi and N. Senthil Kumar

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Abstract

Synthesis and design of a novel substituted morpholine derivatives and evaluation for their anti-cancer activity. The docking study of the designed compound was studied against topoisomerase and the result of docking studies revealed that all compoundspossess significant to moderate interaction with the target enzyme. Amongthese compounds are subjected to in-vitro cytotoxicity study by SRB assay method with cell lines MDA-MB-231 cell lines. All the tested compounds displayed an IC50> 115 μg/mL at a concentration range of 30–250 μg/mL. Among the tested compounds, derivative M5 substituted with methoxy shows a significant IC50 value (81.92 μg/ml) and followed by compound M2 substituted with methyl derivative (88.27 μg/ml) shows good inhibition in the breast cancer cell line.Remaining all other tested compounds shows well to moderate cytotoxic activity on the tested cell line.

Keywords: Docking study, topoisomerase II, Docking study, in-vitro studies, MDA-MB-231, cytotoxic activity.