Synthesis and Anticancer Activity of N-(di/trimethoxyaryl)-5-arylisoxazole-3-carboxamide

Abstract

In this study, a new series of N-(di or trimethoxyaryl)-5-arylisoxazole-3-carboxamide derivatives were synthesized and evaluated against human breast cancer cell lines including MCF-7, MDA-MB-231, and T-47D. Among the synthesized compounds, 5-(m-tolyl)-N-(3,4,5-trimethoxyphenyl)isoxazole-3-carboxamide (8f) showed significant cytotoxicity against all three cell lines comparing with etoposide as the reference drug. Also, Annexin V-FITC/propidium iodide and acridine orange/ethidium bromide staining assay were performed to validate apoptotic activity of compound 8f. The results confirmed induction of apoptosis at early stage.

Keywords:

• Anticancer
• apoptosis assay
• arylisoxazole
• carboxamide
• isoxazole
• synthesis

Funding

This work was supported by grants from the Research Council of Tehran University of Medical Sciences with project No. 94-01-33-28714.