|
|||||
|
|
N(4)-tolyl-2-benzoylpyridine-derived thiosemicarbazones and their palladium(II) and platinum(II) complexes: Cytotoxicity against human solid tumor cells |
|
| Authors: | Karina OS FerrazGabriele MM Cardoso Caryne Margotto BertolloElaine M Souza-Fagundes Nivaldo SpezialiCarlos L Zani Isolda C MendesMaria A Gomes Heloisa Beraldo |
| Institution: | a Departamento de Química, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, Brazil b Departamento de Fisiologia e Biofísica, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, Brazil c Departamento de Física, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, Brazil d Centro de Pesquisas Rene Rachou, Fiocruz, Av Augusto de Lima 1715, Belo Horizonte, Brazil e Departamento de Parasitologia, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, Brazil |
| Abstract: | Complexes Pt(2Bz4oT)Cl], Pt(2Bz4mT)Cl], and Pt(2Bz4pT)Cl] were prepared with N(4)-ortho-(H2Bz4oT), N(4)-meta-(H2Bz4mT), and N(4)-para-(H2Bz4pT) tolyl-2-benzoylpyridine-derived thiosemicarbazones. The thiosemicarbazones exhibited moderate anti-proliferative activity against HepG2 (hepatoma) and UACC-62 (melanoma) cancer cell lines, but showed high anti-proliferative effect against A431 (epithelial carcinoma) cancer cell lines. Upon coordination to platinum(II) the anti-proliferative activity decreases in all cases. The cytotoxicity of the previously prepared palladium(II) analogues Pd(2Bz4oT)Cl], Pd(2Bz4mT)Cl], and Pd(2Bz4pT)Cl] was also investigated. As in the case of the platinum(II) complexes, coordination to palladium(II) did not lead to activity improvement. Investigations on the mechanism of cytotoxic action against A431 cells revealed that Pd(2Bz4oT)Cl] induced DNA fragmentation and apoptosis while H2Bz4oT did not present this effect. The high anti-proliferative effect of the thiosemicarbazones and Pd(2Bz4oT)Cl] against A431 cells, together with the pro-apoptotic effect of Pd(2Bz4oT)Cl] suggests that these compounds have potential as chemotherapeutic drug candidates. |
| Keywords: | Thiosemicarbazones Platinum(II) complexes Solid tumor |
| 本文献已被 ScienceDirect 等数据库收录！ | |