Epidermal Growth Factor Receptor (EGFR) tyrosine kinase inhibitors are widely used for non-small cell lung cancer (NSCLC) therapy. Unfortunately, patients with NSCLC with EGFR mutations developed disease progression after treatment with geftinib for 10-14 months.<br/>To study the possibility of overcoming the resistance of lung cancer cells to gefitinib, we synthesized a series of new 5-cyanopyrimidine derivatives and analyzed the induction of cytotoxic activity and apoptosis using flow cytometry. For this, we synthesized a library of compounds based on the 5-cyanopyrimidine scaffold containing 48 compounds, and the cytotoxic activity of all compounds in vitro was screened for cancer cell lines A549 and A549 resistant to gefitinib (A549GR) by the MTT assay. The results showed that all compounds showed a certain degree of inhibition (IC50) of A549 cancer cells in the range of 3.9–46.56 μM, in which compounds SV296 and SV350 showed pronounced cytotoxic activity against both cell lines. The SV296 and SV350 compounds on A549GR cells showed a decrease in the number of living cells to 50.02% and 62.43% after 24h of incubation, respectively. Gefitinib did not cause a pronounced decrease in the number of living cells on A549GR cells. A549 that were treated with IC50 concentrations of SV296 and SV350 demonstrated a slight decrease in in the number of living cells to 84.96% and to 89.15% for SV350.

Novel 5-cyanopyrimidine based compounds overcome induced gefitinib resistance on a549 cancer cell

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.