Two water-soluble molybdenocene complexes containing oxygen chelating ligands, maltolato and malonate, have been synthesized to elucidate the role of the ancillary ligands in the molybdenocene cytotoxic activity. The structural characterizations of these species by 1 H NMR and IR spectroscopies suggest that both molybdenocene complexes contain the ligands in a bidentate fashion and elemental analysis and mass spectrometry corroborate the proposed formula for the species to be Cp 2 Mo (malonate) and [Cp 2 Mo(maltolato)]Cl (Cp is cyclopentadienyl). Metal-albumin binding studies were pursued using UV-vis spectroscopy and cyclic voltammetric techniques. Whereas metalalbumin binding studies using UV-vis spectroscopy did not show any evidence of interaction, cyclic voltammetry experiments showed that molybdenocene complexes may be involved in weak binding interactions with albumin, most likely in hydrophobic interactions. The cytotoxic activities of Cp 2 Mo(malonate) and [Cp 2 Mo(maltolato)]Cl alone with Cp 2 MoCl 2 were investigated in HT-29 colon cancer and MCF-7 breast cancer cell lines using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide cell viability assay. Cp 2 Mo(malonate) and [Cp 2 Mo(maltolato)]Cl showed slight improvement in terms of cytotoxic activity as compared with Cp 2 MoCl 2 in the HT-29 colon cancer cell line, whereas for MCF-7 all the molybdenocene species exhibited a proliferative profile. The molybdenocene-containing chelating ligands showed stronger proliferative effects than Cp 2 MoCl 2 . There is no correlation between the binding affinity of molybdenocenes for human serum albumin and cytotoxic activity toward HT-29 and MCF-7 cancer cells.