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Gallium(III) Complexes With 2-acetylpyridine-derived Thiosemicarbazones: Antimicrobial and Cytotoxic Effects and Investigation on the Interactions With Tubulin

Gallium(III) Complexes With 2-acetylpyridine-derived Thiosemicarbazones: Antimicrobial and Cytotoxic Effects and Investigation on the Interactions With Tubulin

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

Biometals. 2013 Feb;26(1):151-65.

PMID: 23344786

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1122629	2-Acetylpyridine		1122-62-9	Price

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