Synthesis, trypanocidal and cytotoxic activities of α,β-unsaturated ketones derived from eugenol and analogues.
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2022
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This work describes the synthesis, structural characterization, trypanocide and cytotoxic evaluation of α,β-unsaturated
ketones derived from eugenol and analogues. Among the synthesized compounds, the cyclopentanonic/dihydroeugenol
derivative 12 was active against amastigote forms of Trypanosoma cruzi at 5.2 nM (700 times more potent than
benznidazole) and represents a potential hit for future structural optimizations to reduce its toxicity. All the compounds were
also evaluated against a healthy human and four cancer cell lines and the derivative 10 was more active than doxorubicin
against three cancer cells (IC50 values between 2.03–23.51 μM) and showed the higher selectivity index considering the
human cells. Derivative 14 was also more potent and selective than doxorubicin against two cancer cells (IC50 values
between 4.71–8.86 μM).
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Eugenol, Trypanocide activity
Citação
REIS, R. C. F. M. et al. Synthesis, trypanocidal and cytotoxic activities of α,β-unsaturated ketones derived from eugenol and analogues. Medicinal Chemistry Research, v. 31, p. 2152–2159, 2022. Disponível em: <https://link.springer.com/article/10.1007/s00044-022-02976-x>. Acesso em: 01 ago. 2023.