Anticancer Activity of Aminoacid Linked Novel 4-Methylumbelliferone Derivatives

Abstract

Background: Cancer is a disease of high mortality. The therapeutic agents currently available are insufficient to cure it and are associated with serious side effects. 4-methylumbelliferone is a natural product containing benzo-α-pyrones as a central nucleus. Benzo-α-pyrone is a privileged moiety having multifarious biological activities including anticancer activity. A series of compounds were synthesized taking 4-methylumbelliferone as a core nucleus and screened for their anticancer activity against HeLa cancer cell line. Methods: The 4-methylumbelliferone was linked with aminoacids using chloroacetyl chloride or ethyl chloroacetate as linker. The N-methylmorpholine and isobutylchloroformate protocol was used for amidic coupling. The final compounds were tested against the HeLa cancer cell lines using SRB assay protocol. Results: Three compounds have shown significant anticancer activity viz 9a, 12f and 15l having GI50 (µg/ml) value of, 56.1, 30.9 and 50.9, respectively. Other compound 9f and 13 showed weak anticancer activity having GI50 (µg/ml) value of 97.2 and 71.1, respectively. Conclusion: It has been found that the synthesized derivatives have inhibitory effect on the growth of cancer cell line. Compound 12f has been found as the most active compound of the synthesized series.