ANTIPROLIFERATIVE ACTIVITY OF NEW 6-BROMINE DERIVATIVES OF 7-ANILINO-1-ARYLISOQUINOLINEQUINONES
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 &...
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Sociedad Chilena de Química
2016
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oai:scielo:S0717-970720160004000082017-01-16ANTIPROLIFERATIVE ACTIVITY OF NEW 6-BROMINE DERIVATIVES OF 7-ANILINO-1-ARYLISOQUINOLINEQUINONESIBACACHE,JUANA ANDREAVALDERRAMA,JAIME AARANCIBIA,VERÓNICATHEODULOZ,CRISTINAMUCCIOLI,GIULIO GBENITES,JULIO Isoquinolinequinones half-wave potentials MTT assay antiproliferative activity 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.info:eu-repo/semantics/openAccessSociedad Chilena de QuímicaJournal of the Chilean Chemical Society v.61 n.4 20162016-12-01text/htmlhttp://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072016000400008en10.4067/S0717-97072016000400008 |
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Scielo Chile |
collection |
Scielo Chile |
language |
English |
topic |
Isoquinolinequinones half-wave potentials MTT assay antiproliferative activity |
spellingShingle |
Isoquinolinequinones half-wave potentials MTT assay antiproliferative activity IBACACHE,JUANA ANDREA VALDERRAMA,JAIME A ARANCIBIA,VERÓNICA THEODULOZ,CRISTINA MUCCIOLI,GIULIO G BENITES,JULIO ANTIPROLIFERATIVE ACTIVITY OF NEW 6-BROMINE DERIVATIVES OF 7-ANILINO-1-ARYLISOQUINOLINEQUINONES |
description |
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. |
author |
IBACACHE,JUANA ANDREA VALDERRAMA,JAIME A ARANCIBIA,VERÓNICA THEODULOZ,CRISTINA MUCCIOLI,GIULIO G BENITES,JULIO |
author_facet |
IBACACHE,JUANA ANDREA VALDERRAMA,JAIME A ARANCIBIA,VERÓNICA THEODULOZ,CRISTINA MUCCIOLI,GIULIO G BENITES,JULIO |
author_sort |
IBACACHE,JUANA ANDREA |
title |
ANTIPROLIFERATIVE ACTIVITY OF NEW 6-BROMINE DERIVATIVES OF 7-ANILINO-1-ARYLISOQUINOLINEQUINONES |
title_short |
ANTIPROLIFERATIVE ACTIVITY OF NEW 6-BROMINE DERIVATIVES OF 7-ANILINO-1-ARYLISOQUINOLINEQUINONES |
title_full |
ANTIPROLIFERATIVE ACTIVITY OF NEW 6-BROMINE DERIVATIVES OF 7-ANILINO-1-ARYLISOQUINOLINEQUINONES |
title_fullStr |
ANTIPROLIFERATIVE ACTIVITY OF NEW 6-BROMINE DERIVATIVES OF 7-ANILINO-1-ARYLISOQUINOLINEQUINONES |
title_full_unstemmed |
ANTIPROLIFERATIVE ACTIVITY OF NEW 6-BROMINE DERIVATIVES OF 7-ANILINO-1-ARYLISOQUINOLINEQUINONES |
title_sort |
antiproliferative activity of new 6-bromine derivatives of 7-anilino-1-arylisoquinolinequinones |
publisher |
Sociedad Chilena de Química |
publishDate |
2016 |
url |
http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072016000400008 |
work_keys_str_mv |
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1714200900949508096 |