The invention belongs to the technical field of medicinal chemistry, and particularly relates to a glycosyl modified naphthalimide-polyamine conjugate as well as a preparation method and application thereof. According to the invention, a naphthalimide mother nucleus is modified by glycosyl groups such as peracetyl or deprotected glucose, galactose, mannose, rhamnose, maltose, lactose, cane sugar and the like, so that the glycosyl transporter (GLUTs) with high expression of targeted tumor cells is realized, and better targeting on liver cancer and advanced liver cancer is realized. The novel naphthalimide-polyamine conjugate targeting liver cancer and advanced liver cancer is found for the first time, the naphthalimide complex capable of regulating subcellular organelles is found for the first time, and a new thought and a research direction are provided for treatment of the advanced liver cancer.