Publisher Summary This chapter discusses that the consideration of the status of chemotherapy of cancer in man today is based upon the actual achievement of objective effects against several forms of disseminated cancer by the action of chemical substances. A review of the advances in cancer chemotherapy in small number of institutions, which have pioneered in this field, leaves no question concerning the value of these directions of research. The chapter explores that the panels are accelerating progress in the areas of organic chemistry, screening, pharmacology, biochemistry, and clinical investigation. Synthesis of new chemical compounds is proceeding in a number of directions, although most of the workers are making nucleic acid inhibitors and cytotoxic agents. The pharmaceutical industry and the university laboratories are furnishing thousands of chemical compounds for biological studies from their stock sources. The chapter concludes that the costly lag between discovery in the laboratory or in the clinic and application to the patient with cancer should be abolished or greatly shortened.