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Springer (part of Springer Nature), BioMetals, 1(26), p. 151-165

DOI: 10.1007/s10534-012-9603-1

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

Journal article published in 2013 by 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 ORCID
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This paper is available in a repository.

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Abstract

Complexes [Ga(2Ac4pFPh)(2)]NO(3) (1), [Ga(2Ac4pClPh)(2)]NO(3) (2), [Ga(2Ac4pIPh)(2)]NO(3) (3), [Ga(2Ac4pNO(2)Ph)(2)]NO(3)·3H(2)O (4) and [Ga(2Ac4pT)(2)]NO(3) (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-(H2Ac4pNO(2)Ph) 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.