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Antiproliferative activity of new 6-bromine derivatives of 7-anilino-1-arylisoquinolinequinones

Ibacache, Juana Andrea;Valderrama, Jaime A;Arancibia, Verónica;Theoduloz, Cristina;Benites, Julio;et.al.
(2016) Journal of the Chilean Chemical Sociaty — Vol. 61, n° 4, p. 3191-3194 (2016)

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Authors
  • Ibacache, Juana Andrea
    Author
  • Valderrama, Jaime A
    Author
  • Arancibia, Verónica
    Author
  • Theoduloz, Cristina
    Author
  • Author
  • Benites, Julio
    Author
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Abstract
A variety of 6-bromine-containing 7-anilino-1-arylisoquinolinequinones 2a-g were synthesized to evaluate their half-wave potentials and in vitro antiproliferative activity on gastric and leukemia cancer cell lines. The new compounds displayed significant IC50 values in the range: 1.31 to 11.04 μM. The structure activity relationship analysis of the new series suggest that the antiproliferative activity is dependent, in part, on the push-pull electronic effects of the nitrogen and bromine substituents inserted into the redox fragment of the 1-arylisoquinolinequinone scaffold. Linear regression analysis provided satisfactory relationships between the log IC50 and ClogP values for the AGS gastric cancer cell line.
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Citations

Ibacache, J. A., Valderrama, J. A., Arancibia, V., Theoduloz, C., Muccioli, G., & Benites, J. (2016). Antiproliferative activity of new 6-bromine derivatives of 7-anilino-1-arylisoquinolinequinones. Journal of the Chilean Chemical Sociaty, 61(4), 3191-3194. https://doi.org/10.4067/S0717-97072016000400008 (Original work published 2016)