Anticancer Activity and DNA Binding Studies of Novel 3,7‐Disubstituted Benzopyrones

We have designed and synthesized novel 7-substituted-3-acetyl-benzopyrones 9 a-9 g and ethyl 7-substituted-3-carboxylate-benzopyrones 10 a-10 d and screened for anticancer activity using MTT assay. Most of the tested compounds have shown very good activity against A549 cell line (lung cancer cell-line) and MCF7 cell line (breast cancer cell-line) compared to 5-Fluorouracil. Compound 9 b and 9 e exhibited excellent anticancer activity with IC50 0.16 nM against A549 cell line and 84.8 nM against MCF7 cell line respectively. Compounds 9 b and 9 e showed excellent anticancer activity at very low concentration, well falling in nanomolar region. Compounds 9 b and 9 e exhibited very good binding constant for DNA binding through intercalation in UV based DNA titration which was further confirmed by fluorescence based EtBr displacement assay in DNA-EtBr complex.