Two diaminobis(phenolato) Ti(IV) complexes were separately combined with azatoxin, camptothecin or cisplatin and underwent in vitro cytotoxicity analysis toward HT-29 and NCI-H1229 cancer cell lines. The methylated salan derivative exhibited synergistic effects with cisplatin at varying ratios toward both lines, when the compounds were administered fresh and simultaneously, implying great medicinal potential.