A new series of titanocene dichloride derivatives bearing cyclic alkylammonium groups: Assessment of their cytotoxic properties

Ten new water soluble titanocene dichloride derivatives have been synthesized and characterized and their cytotoxicities against the human lung cancer cell line A549 have been assessed. The potencies of the compounds vary greatly, but dicationic 3-picolylium and 4-picolylium compounds exhibit IC50 values that are unusually low for this class of compounds. In view of their potency against A549 cells, three of the new complexes were tested further on additional human cell lines including the small cell lung cancer cell line H69, the widely used cervical carcinoma cell line HeLa, the ovarian carcinoma cell line A2780 and its cisplatin resistant derivative A2780/CP. All three compounds exhibited potencies in all cell lines comparable to or better than those observed with the A549 cells, while one complex is actually more potent than cisplatin for HeLa cells.

Ten new water soluble titanocene dichloride derivatives have been synthesized and characterized and their cytotoxicities against the human lung cancer cell line A549 have been assessed. The potencies of the four compounds vary greatly, but the dicationic 3-picolylium and 4-picolylium compounds, 6b and 7b, exhibit IC50 values that are unusually low for this class of compounds.Figure optionsDownload as PowerPoint slide