Both the conjugate and its parent building blocks were characterized by a toolbox of in vitro techniques, which allowed us to conclude that despite the conjugate no longer retaining the ability of the parent drug to cross the BBB or inhibit AChE, it displays significant cytotoxic action against two cancer cell lines, namely breast (MCF-7) and neuroblastoma (SH-SY5Y) cells. The gene discussed is ACHE; the disease is cancer.