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.
Letters in Drug Design & Discovery
Title:Synthesis of 1,1’-Ferrocene Diformates Bearing Isoxazole Moiety and Preliminarily Cytotoxicity to A549, HCT116 and MCF-7 Cell Lines
Volume: 15 Issue: 11
Author(s): Jianping Yong*, Mingxue Yang, Canzhong Lu*Xiaoyuan Wu
Affiliation:
- Xiamen Institute of Rare-earth Materials, Chinese Academy of Sciences, Xiamen 361021,China
- Fujian Institute of Research on the Structure of Matter, Chinese Academy of Sciences, Fuzhou 350002,China
Keywords: 1, 1`-ferrocene diformates, isoxazole moiety, synthesis, structural characterization, antitumor activity, cell lines.
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.
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Cite this article as:
Yong Jianping*, Yang Mingxue , Lu Canzhong *, Wu Xiaoyuan , Synthesis of 1,1’-Ferrocene Diformates Bearing Isoxazole Moiety and Preliminarily Cytotoxicity to A549, HCT116 and MCF-7 Cell Lines, Letters in Drug Design & Discovery 2018; 15 (11) . https://dx.doi.org/10.2174/1570180815666180306124920
DOI https://dx.doi.org/10.2174/1570180815666180306124920 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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