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

• JUANA ANDREA IBACACHE ^[1] ; JAIME A VALDERRAMA ^[2] ; VERÓNICA ARANCIBIA ^[3] ; CRISTINA THEODULOZ ^[4] ; GIULIO G MUCCIOLI ^[5] ; JULIO BENITES ^[2]
  1. [1] Universidad de Santiago de Chile Facultad de Química y Biología
  2. [2] Universidad Arturo Prat Facultad de Ciencias de la Salud
  3. [3] Pontificia Universidad Católica de Chile Facultad de Química
  4. [4] Universidad de Talca Facultad de Ciencias de la Salud
  5. [5] Université Catholique de Louvain Louvain Drug Research Institute Bioanalysis and Pharmacology of Bioactive Lipids Laboratory

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• Localización: Journal of the Chilean Chemical Society (Boletín de la Sociedad Chilena de Química), ISSN-e 0717-6309, ISSN 0366-1644, Vol. 61, Nº. 4, 2016, págs. 3191-3194
• Idioma: inglés
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  • 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.