Synthesis of epoxyazadiradione-thiazole hybrid derivatives and evaluation of their cytotoxic activities.

Abstract

In an attempt to develop natural product-based anticancer agents, a series of novel epoxyazadiradione-thiazole hybrids (6a-j) were synthesised and evaluated for their anticancer activity. All the synthesised derivatives were assessed for in vitro cytotoxic activity against a panel of human cancer and normal cell lines and the results showed that most of the compounds exhibited significant cytotoxic activity against cancer cells and as well some of the compounds showed less cytotoxicity against normal cells. In particular, compound 4 showed potent cytotoxic activity against tongue cancer cell lines. In consideration of the potent activity, the compound 4 was further assessed for cell cycle analysis and the results showed that the compound arrests the cell cycle progression at the G0/G1 phase in the tongue cancer cell lines. Consequently, the annexin V/PI staining assay demonstrated that compound 4 induced early apoptosis against tongue cancer. Taken together, the results inferred that the epoxyazadiradione is promising anticancer candidate for developing novel anticancer drugs against tongue cancer.