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DOI: 10.1055/a-2500-9552
Oxaprozin and SB-431542 Hybrid Molecule Inhibits Fibrosis and Cancer Cell Migration
This work was supported by a Grant-in-Aid for Scientific Research (B) from the Japan Society for the Promotion of Science (17H03999) (to M. O.) and a grant for the Joint Research Project with Science Farm Ltd.


Abstract
In this study, we synthesized a novel oxaprozin and SB-431542 hybrid molecule, AF-3, exhibiting antifibrotic and anti-cell-migration activities. Although oxaprozin was expected to exhibit antifibrotic activity, this was not observed in this study. Therefore, we designed AF-3 as an oxaprozin derivative and obtained its synthetic precursor, AF-2. Carboxylic acid AF-2 and carboxamide AF-3 showed similar inhibitory activities against AKT phosphorylation and expression of the mesenchymal cell marker, vimentin. Notably, AF-2 exerted weaker effects on cell migration and fibrosis than AF-3. Although the underlying mechanisms remain elusive, this study provides valuable insights for the development of new drugs against fibrosis and cancer metastasis related to cell migration.
Key words
oxaprozin - SB-431542 - hybrid molecule - anti-fibrotic activity - anti-cell migration activity - vimentin - AKTSupporting Information
- Supporting information for this article is available online at https://doi.org/10.1055/a-2500-9552.
- Supporting Information
Publication History
Received: 13 October 2024
Accepted after revision: 11 December 2024
Accepted Manuscript online:
11 December 2024
Article published online:
21 January 2025
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