1. Microwave synthesis of coumarin-maltol hybrids as potent antitumor and anti-microbial drugs: An approach to molecular docking and DNA cleavage studies
- Author
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Kallappa M. Hosamani, Shrinivas Koparde, Delicia A. Barretto, and Shrinivas D. Joshi
- Subjects
chemistry.chemical_classification ,Gel electrophoresis ,biology ,010405 organic chemistry ,Maltol ,General Chemistry ,Coumarin ,biology.organism_classification ,01 natural sciences ,In vitro ,0104 chemical sciences ,HeLa ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Enzyme ,chemistry ,Biochemistry ,030220 oncology & carcinogenesis ,Cancer cell ,DNA - Abstract
A series of new coumarin-maltol hybrids (2a–2k) were selectively prepared in high yields under microwave irradiation. All the newly synthesized compounds were characterized by elemental and spectroscopic analysis. The synthesized compounds were evaluated for their in-vitro anticancer activity against two human cancer cell lines viz., A-549 (human lung carcinoma) and HeLa (human cervical cancer). Among the tested, compounds (2a) and (2d) were found to be potent cytotoxic with IC50 values in the range of 2.47–4.26 µM on A-549 and HeLa cancer cells. DNA cleavage study by gel electrophoresis method revealed that the compounds (2a), (2j) and (2k) were found to cleave the DNA completely, as no traces of DNA were found. Furthermore, Molecular docking was performed against 4TZK enzyme of E. coli, which showed good binding interactions and is in agreement with the in vitro anti-microbial results.
- Published
- 2018
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