Cytotoxicity studies of coumarin analogs: design, synthesis and biological activity

• Published in: RSC advances 2016-01, Vol.6 (11), p.98816-98828
• Main Authors: Venkata Sairam, K, Gurupadayya, B. M, Vishwanathan, B. Iyer, Chandan, R. S, Nagesha, Dattatri K
• Format: Article
• Language: English
• ISSN: 2046-2069; 2046-2069
• DOI: 10.1039/c6ra22466k

In the present study, a series of coumarin derivatives were designed, synthesized and evaluated for their antioxidant and cytotoxic properties. The title compounds, 2-(3-substituted-4-methyl-2-oxo-2 H -chromen-7-yloxy)-2-methylpropanoic acid derivatives 5a-5f , were synthesized by base-catalyzed dehydrohalogenative cyclization following Hantzsch synthesis. All the newly synthesized analogues were characterized and established on the basis of mass, 1 H NMR, 13 C NMR and IR studies. The compounds were evaluated for their in vitro antioxidant activity and found to exhibit substantial activity. The in vitro cytotoxicity was evaluated against MCF-7, MDA-231 (human breast cancer) and HT29 (human colon adenocarcinoma) cell lines by MTT assay and the results were encouraging. Compound 5b , with lower IC 50 values of 2.4 and 4.8 μM for MCF-7 and MDA-231, respectively, was considered to be potent among the series. In the present study, a series of coumarin derivatives were designed, synthesized and evaluated for their antioxidant and cytotoxic properties.