Premium
Anticancer Activity and DNA Binding Studies of Novel 3,7‐Disubstituted Benzopyrones
Author(s) -
Durgapal Sunil Dutt,
Soni Rina,
Umar Shweta,
Suresh Balakrishnan,
Soman Shubhangi S.
Publication year - 2017
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201601361
Subject(s) - dna , binding constant , cell culture , chemistry , microbiology and biotechnology , intercalation (chemistry) , mtt assay , titration , a549 cell , cell , stereochemistry , biochemistry , binding site , biology , organic chemistry , genetics
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 IC 50 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.