Synthesis, cytotoxic study and docking based multidrug resistance modulator potential analysis of 2-(9-oxoacridin-10(9H)-yl)-N-phenyl acetamides

•Fifteen 2-(9-oxoacridin-10(9H)-yl)-N-phenyl acetamide derivatives were synthesized.•All molecules were screened for anti-cancer activity against three cancer cell lines.•Docking simulation was performed to analyze the MDR modulator potential of molecules.

The present study describes the synthesis of fifteen 2-(9-oxoacridin-10(9H)-yl)-N-phenyl acetamide derivatives (13a–o) through condensation of 2-chloro-N-phenyl acetamides (12a–o) with acridone molecule (10). All the synthesized compounds were screened for their anti-cancer activity against three diverse cell lines including breast (MCF-7), cervical (HeLa) and lung adenocarcinoma (A-549) employing standard MTT assay. Among synthesized molecules, 13k and 13l showed good cytotoxicity activity against considered three cancer cell lines. Additionally, in silico studies of multidrug resistance modulator (MDR) effects of these compounds was performed by docking simulation in the ATP binding site of P-gp. The results of docking simulation displayed important interactions of these molecules in the active site of this protein and predicted their MDR modulator behavior.

Graphical abstractA series of 2-(9-oxoacridin-10(9H)-yl)-N-phenyl acetamide derivatives have been synthesized, screened for anti-cancer activity, and subsequently docked into the ATP binding site of P-gp to predict their multidrug resistance modulator behavior.Figure optionsDownload full-size imageDownload as PowerPoint slide