ANTIPROLIFERATIVE ACTIVITY OF NEW 6-BROMINE DERIVATIVES OF 7-ANILINO-1-ARYLISOQUINOLINEQUINONES

被引：10

作者：

Andrea Ibacache, Juana ^{[1
]}

Valderrama, Jaime A. ^{[2
,3
]}

Arancibia, Veronica ^{[4
]}

Theoduloz, Cristina ^{[5
]}

Muccioli, Giulio G. ^{[6
]}

Benites, Julio ^{[2
,3
]}

机构：

[1] Univ Santiago Chile, Fac Quim & Biol, Casilla 40, Santiago, Chile

[2] Univ Arturo Prat, Fac Ciencias Salud, Casilla 121, Iquique, Chile

[3] Univ Arturo Prat, Inst Ciencias Exactas & Nat, Casilla 121, Iquique, Chile

[4] Pontificia Univ Catolica Chile, Fac Quim, Casilla 306, Santiago, Chile

[5] Univ Talca, Fac Ciencies Salut, Talca, Chile

[6] Catholic Univ Louvain, Louvain Drug Res Inst, Bioanal & Pharmacol Bioact Lipids Lab, B-1200 Brussels, Belgium

来源：

JOURNAL OF THE CHILEAN CHEMICAL SOCIETY | 2016年 / 61卷 / 04期

关键词：

Isoquinolinequinones; half-wave potentials; MTT assay; antiproliferative activity; CYTOTOXIC ISOQUINOLINE QUINONES; CANCER-CELL LINES; BIOLOGICAL EVALUATION; ASSAY; 1,4-NAPHTHOQUINONES; HEPATOCYTES; ANTICANCER; CDC25;

D O I：

10.4067/S0717-97072016000400008

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

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 mu M. 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.

引用

页码：3191 / 3194

页数：4

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