| abstract |
The invention discloses an aromatic nitrogen mustard-mildamine conjugate and its preparation method and medical application. The compound (1) reacts with the compound (2) in the presence of polypeptide condensing agents EDCI and DMAP, or in the presence of HATU and DIPEA Compound I is obtained, which is used to prepare a drug for treating tumors. The invention combines two kinds of drugs with different types of targets to form a prodrug, realizes synergistic anti-tumor effect with multiple actions, improves anti-tumor activity and tolerance, and reduces drug resistance of tumors to drugs. At the same time, the use of amide bonds to link the amines can also reduce the degradation of the amino groups on the benzene rings of the amines by enzymes in vivo, and improve their bioavailability in vivo. |