Abstract: Amooranin (AMR) has been found to cause tumor cell death through G2/M cell cycle arrest, caspase activation, and apoptosis. Furthermore, it has been demonstrated that AMR is a substrate for P-glycoprotein. Based on these activities, AMR compounds, including AMR analogs, can be used in the treatment of a number of diseases in which aberrant cellular proliferation occurs such as drug-sensitive and drug-resistant cancers, autoimmune disorders, and inflammatory diseases.