Gallium(III) complexes with 2-acetylpyridine-derived thiosemicarbazones: antimicrobial and cytotoxic effects and investigation on the interactions with tubulin

被引：0

作者：

Josane A. Lessa

Marcella A. Soares

Raquel G. dos Santos

Isolda C. Mendes

Lívia B. Salum

Hikmat N. Daghestani

Adriano D. Andricopulo

Billy W. Day

Andreas Vogt

Heloisa Beraldo

机构：

[1] Instituto de Química,Departamento de Fisiologia e Biofísica

[2] Universidade do Estado do Rio de Janeiro,Departamento de Química

[3] Centro de Desenvolvimento da Tecnologia Nuclear,Department of Structural Biology

[4] CDTN,Department of Pharmaceutical Sciences

[5] Universidade Federal de Minas Gerais,undefined

[6] Universidade Federal de Minas Gerais,undefined

[7] Centro de Biotecnologia Molecular Estrutural,undefined

[8] Instituto de Física de São Carlos,undefined

[9] Universidade de São Paulo,undefined

[10] University of Pittsburgh,undefined

[11] University of Pittsburgh,undefined

[12] University of Pittsburgh Drug Discovery Institute,undefined

[13] University of Pittsburgh,undefined

来源：

BioMetals | 2013年 / 26卷

关键词：

Thiosemicarbazones; Gallium(III) complexes; Antimicrobial activity; Cytotoxicity; Tubulin;

D O I：

暂无

中图分类号：

学科分类号：

摘要：

Complexes [Ga(2Ac4pFPh)2]NO3 (1), [Ga(2Ac4pClPh)2]NO3 (2), [Ga(2Ac4pIPh)2]NO3 (3), [Ga(2Ac4pNO2Ph)2]NO3·3H2O (4) and [Ga(2Ac4pT)2]NO3 (5) were obtained with 2-acetylpyridine N(4)-para-fluorophenyl-(H2Ac4pFPh), 2-acetylpyridine N(4)-para-chlorophenyl-(H2Ac4pClPh), 2-acetylpyridine N(4)-para-iodophenyl-(H2Ac4pIPh), 2-acetylpyridine N(4)-para-nitrophenyl-(H2Ac4pNO2Ph) and 2-acetylpyridine N(4)-para-tolyl-(H2Ac4pT) thiosemicarbazone. 1–5 presented antimicrobial and cytotoxic properties. Coordination to gallium(III) proved to be an effective strategy for activity improvement against Pseudomonas aeruginosa and Candida albicans. The complexes were highly cytotoxic against malignant glioblastoma and breast cancer cells at nanomolar concentrations. The compounds induced morphological changes characteristic of apoptotic death in tumor cells and showed no toxicity against erythrocytes. 2 partially inhibited tubulin assembly at high concentrations and induced cellular microtubule disorganization, but this does not appear to be the main mechanism of cytotoxic activity.

引用

页码：151 / 165

页数：14

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