No abstract

Cervical cancer seriously threatens women’s health, it seriously harm the patient’s physical and mental health. The new derivative of Acanthus ilicifolius Linn alkaloid 2-benzoxazone was obtained from o-aminophenol, substituted benzaldehyde, trichloroacetic acid and isocyanate via a tandem Ugi 4CC/SN cyclization (N-cyclohexyl-2-(2-benzoxazolone-3-yl)-2-p-trifluoromethylphenylacetamide, BOABB), and the toxicity of the new compound to the cervical cancer C-33A cells was detected by CCK-8 assay, wound healing assay and apoptotic assay. The results exhibited that BOABB had obvious inhibitory effect on C-33A cells, and the calculated IC50 was 32.3 μM. Wound healing assay showed that BOABB could significantly inhibit cell migration (P<0.05). The apoptotic assay demonstrated that BOABB has induced apoptosis in C-33A cells (from 10.86% to 34.70%).

A one-pot, base-mediated approach to Acanthus ilicifolius Linn alkaloid 2-benzoxazolinone derivatives is developed. Starting from trichloroacetic acid, o-aminophenol, substituted benzaldehydes and alkyl isocyanides, the desired 2-benzoxazolinone derivatives are obtained in good yields via a tandem Ugi condensation and intramolecular haloform cyclization at room temperature in the presence of Et3N.