RESUMO
The cytotoxicity of several Co(II), Ni(II), Cu(II) and Zn(II) complexes with various molecular structures and geometries, has been tested on LoVo and 2008 cells at 1-100 microM concentration for 24 h exposure. On the basis of 24 h results, the exposure time was prolonged to 48 and to 72 hours. The most potent complexes result [Cu(tren)(H2O)]2+ 2Cl-, E, [CoCl3(H2Meppz)], G, and [CoCl3(HMe2ppz)], H, (tren=tris(2-aminoethyl)amine, H2Meppz=1-methylpiperazin-1-ium, HMe2ppz=1,4-dimethylpiperazin-1-ium cations). Nevertheless, these complexes are able to induce cell growth reduction of about 50% at highest doses tested (1-100 microM ) and after 72 h exposure.
Assuntos
Antineoplásicos/síntese química , Compostos Heterocíclicos de 4 ou mais Anéis/síntese química , Compostos Organometálicos/síntese química , Piperazinas/síntese química , Adenocarcinoma/patologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Neoplasias do Colo/patologia , Feminino , Compostos Heterocíclicos de 4 ou mais Anéis/química , Compostos Heterocíclicos de 4 ou mais Anéis/farmacologia , Humanos , Estrutura Molecular , Compostos Organometálicos/química , Compostos Organometálicos/farmacologia , Neoplasias Ovarianas/patologia , Oxirredução , Piperazinas/química , Piperazinas/farmacologia , Relação Estrutura-Atividade , Células Tumorais Cultivadas/efeitos dos fármacosRESUMO
Some rigid analogues of flavone-8-acetic acid are described. Direct in vitro toxicity of the synthesised compounds was evaluated towards four tumoral cell lines and the ability of these compounds to stimulate mouse peritoneal macrophages in culture to become tumoricidal (indirect toxicity) was also studied. All compounds were able to induce direct cytotoxicity only at very high concentrations but showed a remarkable indirect activity. In particular compound 4d was able to significantly increase macrophage lytic properties and has been selected for further investigations.