The application discloses EGFR-dependent
small molecule conjugates-1, 3 and 4, a preparation method and application thereof, and belongs to the technical field of biological medicines. The EGFR-dependent
small molecule conjugate-1 disclosed by the application is obtained by introducing an IDO inhibitor D-MT into a
lapatinib structure through reasonable structural modification. A
glutathione S-
transferase inhibitor NBDHEX is introduced into the above structural fragment of the
lapatinib through different connectors to obtain target conjugates-3 and 4. The results show that the conjugates all retain the
inhibitory effect of the parent compounds on EGFR, IDO or GST
enzyme activity, have a strong
inhibitory effect on the proliferation of various types of triple-negative
breast cancer cells, can effectively reverse the
lapatinib-mediated
drug resistance of triple-negative
breast cancer cells, and can be used for preparing antitumor drugs.