Chemotherapy is currently the most important medical modality of treatment of cancer. Several studies have shown that most, if not all, chemotherapeutic agents exert their anticancer activity by inducing apoptosis (programmed cell death). Although successful treatment of some malignancies has been achieved, most of solid tumors are scarcely responsive to chemotherapeutic agents. The progress made in the area of apoptosis has led to the development of several apoptosis stimulators compounds for the control of cancer. A number of compounds able to activate directly apoptosis by acting on molecules involved in the apoptotic pathway, such as TRAIL receptor, caspases and the Bcl-2 family of proteins have been recently developed. Most are still in the preclinical study, but some have already shown promising results. Other recently developed anticancer drugs induce indirectly apoptosis by acting on targets different from that of classic chemotherapeutic drugs. Here, we review the experimental and clinical results of several promising pro-apoptotic anti-cancer compounds.