Synthesis, structural characterization and cytotoxicity of bimetallic chlorogold(I) phosphine complexes employing functionalized phosphinoferrocene carboxamides

摘要

Gold(I) phosphine complexes of the general formula [AuCl(Ph_2PfcCONHY-kP)], where Y is CH_2CO_2Me (7), CH_2CONH_2 (8), CH_2CH_2OH (9), CH(CH_2OH)_2 (10), C(CH_2OH)_3 (11), and CH_2SO_3(HNEt_3) (12), and fc is ferrocene-1,1'-diyl, were prepared from [AuCl(tht)] (tht = tetrahydrothiophene) and the appropriate phosphinoferrocene carboxamides (1e6). The compounds were characterized by spectroscopic and analytical methods, and the molecular structures of 7 and 9 were determined by single-crystal X-ray crystallography. Complexes 7-12 exerted antiproliferative activity against the human ovarian cancer cells in vitro. The IC_(50) values ranged ca. 0.3-3.7 mM for the A2780 cell line, and 3.1-20 mM for the cisplatin resistant cell line A2780R, with complex 7 being the most cytotoxic against both cell types. IC_(50)values for the non-tumorigenic human embryonic kidney (HEK) cells, serving as a measure of a general toxicity, were found in roughly similar ranges, i.e. 0.9-6.8 μM