Abstract
Building on our previous work that discovered 1,2,4-triazole-spirodienone as a promising pharmacophore for anticancer activity, we have further diversified 1,2,4-triazole- spirodienone derivatives and synthesized a series of novel naphthalene-substituted triazole spirodienones to explore their antineoplastic activity. Of these, compound 6a possesses remarkable invitro cytotoxic activity by arresting cell cycle and inducing apoptosis in MDA-MB-231cells. Subsequently, acute toxicity assay showed that 6a at 20mg/kg has no apparent toxicity to the major organ in mice. In addition, compound 6ainvivo suppressed breast cancer 4T1 tumor growth. Taken together, these results indicate that compound 6a may be a potential anticancer agent for further development.
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