Synthesis of 1,1’-Ferrocene Diformates Bearing Isoxazole Moiety and Preliminarily Cytotoxicity to A549, HCT116 and MCF-7 Cell Lines

Author(s): Jianping Yong*, Mingxue Yang, Canzhong Lu*, Xiaoyuan Wu

Journal Name: Letters in Drug Design & Discovery

Volume 15 , Issue 11 , 2018

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Graphical 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.

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Article Details

Year: 2018
Page: [1141 - 1146]
Pages: 6
DOI: 10.2174/1570180815666180306124920
Price: $65

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