Here, the aim of this study was to screen a library of previously synthesized CDXs in a panel of cancer cell lines to identify the most promising compounds for further study as possible chemotherapy drugs, as well as to analyze their effect on parameters, like the mechanism of cell death, cell cycle, and metabolism, and verify whether the compounds under study were substrates of Pgp, one of the main mechanisms of resistance in cancer therapy. The gene discussed is PGP; the disease is cancer.