Human MetAP type 2 (MetAP2) is one of the three known methionine aminopeptidases, linked to several types of cancer, which was the target of the drug discovery project by Weglarz-Tomczak et al. Starting with ebselen, a series of benzisoselenazolone and diselenide derivatives was prepared with compounds 48 and 50 bearing benzyl and 2-chloro-4-methyl phenyl fragments, respectively (Figure 14) resulting in the best-in-class being able to inhibit MetAP2 with a higher potency compared with ebselen [172]. Here, METAP2 is linked to cancer.