Disclosed are N-aryl-isoxazolopyrimidin-4-amines and related compounds thereof, represented by the Formula (I): wherein Ar, R<SUB>1</SUB>-R<SUB>5</SUB>, A, B, D, E, F and H are defined herein. The present invention relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.