Anticancer Activity and DNA Binding Studies of Novel 3,7-Disubstituted Benzopyrones
| Autor: | Sunil Dutt Durgapal, Balakrishnan Suresh, Rina Soni, Shweta Umar, Shubhangi S. Soman |
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| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
A549 cell 010405 organic chemistry Intercalation (chemistry) General Chemistry 01 natural sciences Combinatorial chemistry Fluorescence Binding constant 0104 chemical sciences 03 medical and health sciences chemistry.chemical_compound 030104 developmental biology chemistry Biochemistry Cell culture MTT assay IC50 DNA |
| Zdroj: | ChemistrySelect. 2:147-153 |
| ISSN: | 2365-6549 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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