In order to gain insights into the molecular mechanism underlying the effectiveness of the Acridone derivatives in overcoming the drug resistance in Glioma, Molecular Docking studies have been performed to compare the binding affinities of the three Acridone derivatives with MGMT, P-gp, and MRP proteins which are responsible for conferring resistance to the Glioma cells. The gene discussed is MGMT; the disease is central nervous system cancer.