In its various forms, cancer remains a leading cause of mortality and morbidity worldwide. Thus, it is widely accepted that finding innovative, life-changing drugs and therapeutic regimens is key for successful future cancer therapy. While natural products and synthetic small molecules have historically contributed to the management of different cancer types, it has become apparent that the inherent cytotoxicity of most of these chemical entities yields narrow therapeutic windows. As consequence, several potentially useful drugs have been discontinued from development pipelines or seen limited clinical application.