Design, synthesis and anticancer activity of functionalized spiro-quinolines with barbituric and thiobarbituric acids

A new series of spiro-quinoline compounds have been accomplished by the reaction of barbituric acid or thiobarbituric acid with derivatives of benzisoxazole-5-carbaldehyde or 2-substituted benzaldehyde. These compounds were evaluated for their in vitro cytotoxicity on two mammalian cancer cell lines MCF-7 and KB. The compounds exhibit cytotoxicity against these cell lines in micromolar range. Among the series of compounds, 11(a–j) particularly 11b and 11e showed relatively good activity against both the tested cell lines. Compound 11b was found to exhibit the highest cytotoxic activity with IC50 value 90.2 µM for MCF-7 and 49.8 µM for KB cell line. Flow cytometric analysis study confirmed that these molecules induced cytotoxicity via apoptosis.