Cancer is one of the major life threatening diseases worldwide. The available anticancer drugs have distinct mechanisms of action which may vary in their effects on different types of normal and cancer cells. Screening methods are routinely and extensively used to reduce cost and time of drug discovery. The traditional anticancer drug screening methods, including animal experiments and cell-based screening assays. Screening methods for the detection of anticancer activity are of importance in order to find solid tumorspecific agents. The screening and evaluation procedures for the development of anticancer agents indicated that the entire process is a rather difficult task. Presently, active compounds are selected by prescreening and screening against transplanted mouse tumors and human tumor xenografts as well as by the in vitro systems. The US National Cancer Institute (NCI) 60 human tumour cell line anticancer drug screen (NCI60) was developed in the late 1980s as an in vitro drug-discovery tool intended to supplant the use of transplantable animal tumours in anticancer drug screening. This screening model give information about the mechanisms of growth inhibition and tumour-cell kill. Recently, its role has changed to that of a service screen supporting the cancer research community. Target-based and cell-based screenings for new anticancer drugs in the molecular targeting period are methods of identifying more selective anticancer drugs. Here I review the development, use and productivity of the screen, highlighting several outcomes that have contributed to advances in cancer chemotherapy. Finally, we discuss primary and secondary in vivo evaluation in experimental chemotherapy.