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

作者：Durgapal Sunil Dutt; Soni Rina; Umar Shweta; Suresh Balakrishnan; Soman Shubhangi S^*

来源：ChemistrySelect, 2017, 2(1): 147-153.

DOI：10.1002/slct.201601361

• Anticancer
• DNA Binding
• Ethyl 7-substituted-3-carboxylate-benzopyrone
• 7-Substituted-3-acetyl-benzopyrone

We have designed and synthesized novel 7-substituted-3acetyl-benzopyrones 9a-9g and ethyl 7-substituted-3-carboxylate-benzopyrones 10a-10d 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 9b and 9e exhibited excellent anticancer activity with IC50 0.16 nM against A549 cell line and 84.8 nM against MCF7 cell line respectively. Compounds 9b and 9e showed excellent anticancer activity at very low concentration, well falling in nanomolar region. Compounds 9b and 9e 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.

• 出版日期2017-1-10