Cancer is still responsible for many deaths worldwide. Apart from prevention, the best solution for cancers remains early detection and cure or treatment. The need for new, effective, relatively safer and affordable remedies for cancer is still paramount. Research into plants as a source of bioactive compounds has increased in recent years. Croton membranaceus is among plants used as herbal remedies in Ghana for the treatment of cancers generally called ?kokram? (Twi). This work sought to establish a scientific basis for the justification and validation of the use of these species especially C. membranaceus for cancers. The investigations established a comprehensive bioactivity profile for the plant. The procedures and techniques used in this book and the revealed useful bioactive compounds in C. membranaceus will be of profound significance to the Naturalists, Traditional Medicine Practitioners, Natural Product Scientists and all those who are using or contemplating research into C. membranaceus. Synthetic Chemists and drug development agents may find information on the cytotoxic novel ?crotomembranafuran? as a useful template for developing more active anticancer analogs.