AI Article Synopsis
- Most zinc metalloproteases are key players in tumor growth and spread, making them important targets for cancer treatment.
- Researchers have developed new compounds called β-dicarbonyl derivatives to specifically inhibit aminopeptidase N (APN/CD13), which is linked to tumor progression.
- Among the tested compounds, 5c showed the strongest inhibitory effect, highlighting its potential as a lead compound for future anti-tumor drug development focused on zinc metalloproteases.
Article Abstract
Most zinc metalloproteases are over-expressed in tumor cells and play a critical role in the genesis, development, and metastasis of tumors. Novel zinc binding groups (ZBGs) represent a novel strategy to obtain optimal potency and selectivity for zinc metalloproteases inhibitors. Here we described the design, synthesis, and biological studies of novel β-dicarbonyl derivatives as aminopeptidase N (APN/CD13) inhibitors. The results demonstrated that some compounds exhibited moderate to good inhibitory activities against APN with compound 5c being the most potent, suggesting that 5c could serve as new lead for the future APN inhibitor development. The results further confirm our design rationale of β-dicarbonyl moiety as a new ZBG, which may provide a new direction for the design and discovery of zinc metalloproteases inhibitors as new anti-tumor agents.
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| http://dx.doi.org/10.1016/j.bmcl.2013.06.058 | DOI Listing |
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