The present application relates to the technical field of biological
medicine, and specifically discloses a small-molecule
coupling compound targeting ASGPR, which has the following general formula: wherein X is a small-molecule ligand with the ability to target ASGPR; and Y is a derivative of
cucurbitacin B. . The small-molecule
coupling compound can be used in the preparation of a
drug targeting ASGPR and having the functions of precise
chemotherapy and radiotherapy
sensitization. The small-molecule
coupling compound prepared by the present application can achieve precise killing of
liver cancer cells; the water
solubility of
cucurbitacin B is improved after coupling; the small-molecule coupling compound integrates precise
chemotherapy and radiotherapy
sensitization, and can significantly enhance the
cancer-killing effect in combination with low-
dose radiotherapy; and the small-molecule coupling compound has no obvious
systemic toxicity and is well tolerated by patients.