Synthesis, Characterization and Evaluation of in vitro Antitumor Activities of Novel Chalcone-Quinolinone Hybrid Compounds
| Autor: | Manoel Odorico de Moraes, Giulio D. C. D’Oliveira, Caridad N. Perez, Luciano M. Lião, Andrea F. Moura |
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| Jazyk: | angličtina |
| Rok vydání: | 2018 |
| Předmět: |
Antitumor activity
Reaction conditions chacone sulfonamide Chalcone 010405 organic chemistry chalcone-quinolinone hybrids Electrospray ionization Single step General Chemistry 010402 general chemistry 01 natural sciences Combinatorial chemistry In vitro 0104 chemical sciences chemistry.chemical_compound chemistry Bromide antitumor activity Claisen-Schmidt condensation IC50 |
| Zdroj: | Journal of the Brazilian Chemical Society, Volume: 29, Issue: 11, Pages: 2308-2325, Published: NOV 2018 Journal of the Brazilian Chemical Society v.29 n.11 2018 Journal of the Brazilian Chemical Society Sociedade Brasileira de Química (SBQ) instacron:SBQ |
| Popis: | Chalcone-quinolinone hybrid compounds, as well as the synthesis of such compounds, have few reports in the literature. Such compounds may be quite useful in therapeutics, since various biological activities are reported for both chalcones and quinolinones. In the present work, several novel chalcone-quinolinone compounds have been synthesized. The reaction conditions developed allowed to obtain the compounds in a single step of synthesis from the chalcones. The products precipitated pure and were isolated by filtration. The yields of such reactions, from 45 to 94%, were promising. The product structures were confirmed by nuclear magnetic resonance (NMR) and electrospray ionization mass spectrometry (ESI-MS) techniques. Their antitumor activities were evaluated in HCT-116 (colon) cell lines by the 3-(4,5-dimethyl-2-thiazole)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) test. The half maximal inhibitory concentration (IC50) values obtained for the most active chalcones were between 2.9 and 7.5 and for active quinolinone was 19.3 mg L-1. The antitumor activities results suggest that the class of compounds studied has potential for use in cancer research. |
| Databáze: | OpenAIRE |
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