作者: Karina S. O. Ferraz , Jeferson G. Da Silva , Flávia M. Costa , Bruno M. Mendes , Bernardo L. Rodrigues
DOI: 10.1007/S10534-013-9639-X
关键词: Mode of action 、 Semicarbazone 、 Cytotoxicity 、 Platinum 、 Thioredoxin reductase 、 2-Acetylpyridine 、 Stereochemistry 、 Chemistry 、 Cisplatin 、 Auranofin 、 General Biochemistry, Genetics and Molecular Biology 、 General Agricultural and Biological Sciences 、 Metals and Alloys 、 Biomaterials
摘要: Complexes [Au(2Ac4oT)Cl][AuCl2] (1), [Au(Hpy2Ac4mT)Cl2]Cl·H2O (2), [Au(Hpy2Ac4pT)Cl2]Cl (3), [Pt(H2Ac4oT)Cl]Cl (4), [Pt(2Ac4mT)Cl]·H2O (5), [Pt(2Ac4pT)Cl] (6) and [Pt(L)Cl2OH], L = 2Ac4mT (7), 2Ac4oT (8), 2Ac4pT (9) were prepared with N(4)-ortho- (H2Ac4oT), N(4)-meta- (H2Ac4mT) N(4)-para- (H2Ac4pT) tolyl-2-acetylpyridine thiosemicarbazone. The cytotoxic activities of all compounds assayed against U-87 T-98 human malignant glioma cell lines. Upon coordination cytotoxicity improved in 2, 5 8. In general, the gold(III) complexes more than those platinum(II,IV). Several these proved to be active cisplatin auranofin used as controls. probably act by inhibiting activity thioredoxin reductase enzyme whereas mode action platinum(II,IV) involves binding DNA. Cells treated studied presented morphological changes such shrinkage blebs formation, which indicate death apoptosis induction.