In view of the lack of anti-cancer targeted drugs in the prior art, the invention provides a naphthylamine compound and a biologically acceptable salt thereof, a preparation method thereof, and an application thereof. The naphthylamine compound and the biologically acceptable salt thereof provided by the invention can bind to protein sites related to tumor diseases in organisms through functional groups in the structure, and have hydrogen bonds and hydrophobic interactions with receptors, so as to achieve the purpose of inhibiting tumor cell proliferation.