Journal
BIOMETALS
Volume 26, Issue 1, Pages 151-165Publisher
SPRINGER
DOI: 10.1007/s10534-012-9603-1
Keywords
Thiosemicarbazones; Gallium(III) complexes; Antimicrobial activity; Cytotoxicity; Tubulin
Categories
Funding
- CNPq
- INCT-INOFAR [Proc. CNPq 573.364/2008-6]
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Complexes [Ga(2Ac4pFPh)(2)]NO3 (1), [Ga(2Ac4pClPh)(2)]NO3 (2), [Ga(2Ac4pIPh)(2)]NO3 (3), [Ga(2Ac4pNO(2)Ph)(2)]NO3 center dot 3H(2)O (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-(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.
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