Abstract
Background: Ferrocene is a potential pharmacophore for drug design and drug discovery.
Methods: Based on our previous good achievements (Med. Chem. commun., 2014,7,968-972), nineteen novel structures of 1,1’-ferrocene diformates bearing isoxazole moiety (3a-3s) were firstly synthesized in the current work and characterized by 1H NMR, 13C NMR, ESI-MS. Then, their cytotoxicity to A549, HCT116 and MCF-7 cell lines was evaluated using the MTT method.
Results: The results showed that most compounds exhibited higher potent cytotoxicity to A549, HCT116 and MCF-7 cell lines.
Conclusion: Especially, 3b, 3h, 3k, 3l, 3m, 3n, 3o, 3p and 3s simultaneously exhibited stronger inhibitory activity towards A549, HCT116 and MCF-7 cell lines than that of the reference drug cisplatin, which can be regarded as very promising metal-based lead compounds for anticancer agents.
Keywords: 1, 1`-ferrocene diformates, isoxazole moiety, synthesis, structural characterization, antitumor activity, cell lines.
Graphical Abstract