Tumors of various etiology are considered to be one of the most frequent reasons for disorders and death. According to the WHO, cancer is a leading cause of death accounting for 7.6 million deaths (ca. 13 % of all deaths) in 2008.
The present review deals with discoveries, research and development in the field of antineoplastics, spanning substances from yperite derivatives to biological therapy and tyrosine kinase inhibitors. The important milestones of the development of antitumor drugs as well as cancer chemotherapy are mentioned.