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Synthesis and biological evaluation of cytotoxic properties of stilbene-based resveratrol analogs

Tipo de material: TextoTextoSeries ; European Journal of Medicinal Chemistry, 44(2), p.701-707, 2009Trabajos contenidos:
  • Rotta, R
  • Marques, M.R
  • Montenegro, R.C
  • Vasconcellos, M.C
  • Pessoa, C
  • De Moraes M.O
  • Costa-Lotufo L.V
  • Costa-Lotufo L.V
  • Nogueira Eberlin, M
Tema(s): Recursos en línea: Resumen: This work deals with the preparation of stilbene-based resveratrol analogs by employing the Perkin reaction, aiming at synthesizing potential antitumor lead compounds and evaluating their pharmacological activities. The proliferation inhibitor test against tumor cell lines identified analogs 9 and 11 as the most active among all synthesized derivatives, presenting IC50 in micromolar range for certain cell lines. For study on the embryonic development, compounds 8 and 9 at the lowest tested concentration (41.7 mM)that inhibited sea urchin egg development, but only after third cleavage were used. Both the compounds inhibited 100 percent of normal development since first cleavage. These data partially corroborated the results obtained with MTT assay using tumor cell lines. None of the tested compounds revealed hemolytic action in assay with mouse erythrocytes.
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This work deals with the preparation of stilbene-based resveratrol analogs by employing the Perkin reaction, aiming at synthesizing potential antitumor lead compounds and evaluating their pharmacological activities. The proliferation inhibitor test against tumor cell lines identified analogs 9 and 11 as the most active among all synthesized derivatives, presenting IC50 in micromolar range for certain cell lines. For study on the embryonic development, compounds 8 and 9 at the lowest tested concentration (41.7 mM)that inhibited sea urchin egg development, but only after third cleavage were used. Both the compounds inhibited 100 percent of normal development since first cleavage. These data partially corroborated the results obtained with MTT assay using tumor cell lines. None of the tested compounds revealed hemolytic action in assay with mouse erythrocytes.

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