Since there is currently no cure for most forms of disseminated cancer, the development of novel active chemotherapeutic drugs is essential. Small molecules are interesting drug candidates as they are able to target important molecular pathways with selectivity. An in-depth analysis of the SAR study and the available preclinical and clinical data can greatly assist in the development of the next generation of anticancer drugs that would be more potent, selective, and would interfere with fewer side effects.