AI Article Synopsis
- A new chemotherapy drug called AG11 was developed from a flavanone derivative and shown to potentially improve survival in advanced bladder cancer patients.
- In lab tests, AG11 had an IC50 of 4.6 μM, causing cell cycle arrest in RT4 cells and promoting apoptosis after 48 hours.
- The drug interferes with tubulin polymerization and disrupts mitotic spindle formation, indicating its potential as a foundation for new anti-microtubule agents.
Article Abstract
Background: New chemotherapy drugs should be investigated to improve survival of patients with advanced bladder cancer. Here, we report the synthesis and evaluation of AG11, a new flavanone derivative obtained through cyclization of its chalcone precursor CB11.
Materials And Methods: The effect of AG11 on cell viability was evaluated by 3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazolium bromide assay and apoptotic cell death was analyzed by flow cytometry. Finally, the effect of AG11 on tubulin polymerization in vitro and microtubule distribution across the cells was investigated.
Results: AG11 was found to have an IC50 (half-maximal inhibitory concentration) of 4.6 μM and its inhibitory effect on RT4 cells proliferation is associated with a cell-cycle arrest in G2+M phases followed by apoptosis after a 48 h treatment. AG11 prevented polymerization of purified tubulin in a concentration-dependent manner in vitro and disrupted mitotic spindle formation in cells.
Conclusion: AG11 appears to be an attractive scaffold for further development of a structurally simpler new anti-microtubule agents.
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