Find in Library

Breast cancer, especially the aggressive triple-negative subtype, poses a serious health threat to women. Unfortunately, effective targets are lacking, leading to a grim prognosis. Research highlights the crucial role of <i>c-MYC</i> overexpression in this form of cancer. Current inhibitors targeting <i>c-MYC</i> focus on stabilizing its G-quadruplex (G4) structure in the promoter region. They can inhibit the expression of <i>c-MYC</i>, which is highly expressed in triple-negative breast cancer (TNBC), and then regulate the apoptosis of breast cancer cells induced by intracellular ROS. However, the clinical prospects for the application of such inhibitors are not promising. In this research, we designed and synthesized 29 acridone derivatives. These compounds were assessed for their impact on intracellular ROS levels and cell activity, followed by comprehensive QSAR analysis and molecular docking. Compound N<b>8</b> stood out, significantly increasing ROS levels and demonstrating potent anti-tumor activity in the TNBC cell line, with excellent selectivity shown in the docking results. This study suggests that acridone derivatives could stabilize the <i>c-MYC</i> G4 structure. Among these compounds, the small molecule N<b>8</b> shows promising effects and deserves further investigation.