The antitumor activity of 4,4'-bipyridinium amphiphiles

A series of 4,4'-bipyridinium amphiphiles were synthesized and their anticancer activities were further evaluated. MTT assay showed that the cytotoxicity first increased and then decreased with the growth of carbon chains (8-16 C) at both ends of bipyridyl. Specifically, compounds with saturated carbon chains consisting of 13 carbons at both ends of bipyridyl displayed the best cell inhibitory activity with IC₅₀ values in the low-micromolar range, which were even superior to that of cisplatin, against all the tested human cancer cells and cisplatin-resistant A549 cancer cells in vitro. In addition, compound 6 could evidently arrest the G2/M phase of the cell cycle in a dose-dependent manner. Moreover, this study demonstrates the potent performance of compound 6 in cell growth inhibition and apoptosis induction via a conceivable approach of membrane damage.