A New Curcuminoids-Coumarin Derivative: Mechanochemical Synthesis, Characterization and Evaluation of Its In Vitro Cytotoxicity and Antimicrobial Properties

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de Moura, Aniele [UNESP]
Gaglieri, Caroline [UNESP]
Alarcon, Rafael Turra [UNESP]
Ferreira, Laura Teófilo [UNESP]
Vecchi, Rafael [UNESP]
Sanches, Mariana Liessa Rovis
de Oliveira, Rodrigo Cardoso
Venturini, James [UNESP]
da Silva-Filho, Luiz Carlos [UNESP]
Junior Caires, Flávio [UNESP]
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Over the years, several drugs have been developed deriving from plants to investigate possible therapeutic roles. Among them, curcuminoids and coumarins, which, display a wide range of biological activity against several strains. Therefore, it was synthesized a curcuminoids-coumarin derivative by a mechanochemical multicomponent reaction. By NMR and HRMS results confirmed the formation of a mixture of three curcuminoids-coumarin derivatives in the same sample. The Influence of time during the milling process was evaluated, resulting in a crystalline product in only 30 min. The LAG milling carried out with different solvents showed that the product is obtained regardless of the solvent polarity. Furthermore, the biological evaluation showed that the curcuminoids-coumarin derivative has better activity against S. aureus than curcumin and 4-hydroxycoumarin. Lastly, the cell viability study exhibited a decrease of cytotoxicity of the derivative, compared to curcumin, against NIH3T3 cells.
Biological activity, Curcuminoids, Mechanochemistry, Multicomponent reactions, Sustainable chemistry.
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ChemistrySelect, v. 6, n. 41, p. 11352-11361, 2021.