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The biological significance of benzopyran-4-ones as cytotoxic agents against multi-drug resistant cancer cell lines and isoxazoles as anti-inflammatory agents in cellular assays prompted us to design and synthesize their hybrid compounds and explore their antiproliferative activity against a panel of six cancer cell lines and two normal cell lines. Compounds <b>5a</b>–<b>d</b> displayed significant antiproliferative activities against all the cancer cell lines tested, and IC₅₀ values were in the range of 5.2–22.2 μM against MDA-MB-231 cancer cells, while they were minimally cytotoxic to the HEK-293 and LLC-PK1 normal cell lines. The IC₅₀ values of <b>5a</b>–<b>d</b> against normal HEK-293 cells were in the range of 102.4–293.2 μM. Compound <b>5a</b> was screened for kinase inhibitory activity, proteolytic human serum stability, and apoptotic activity. The compound was found inactive towards different kinases, while it completely degraded after 2 h of incubation with human serum. At 5 μM concentration, it induced apoptosis in MDA-MB-231 by 50.8%. Overall, these findings suggest that new benzopyran-4-one-isoxazole hybrid compounds, particularly <b>5a</b>–<b>d</b>, are selective anticancer agents, potentially safe for human cells, and could be synthesized at low cost. Additionally, Compound <b>5a</b> exhibits potential anticancer activity mediated via inhibition of cancer cell proliferation and induction of apoptosis.