The invention relates to nitrogen-atom-containing arteannuin dimers disclosed as Formula (1) and pharmaceutically acceptable salts thereof, wherein X is NR, NR(CH2)nNR or a formula disclosed in the specification; R is H or C14 alkyl group; Y and Z are respectively (CH2)m, (CH2)n(OCH2CH2)m, OC(CH2)nCO or COAr; Ar is phenyl group, naphthyl group or heterocyclic group; N is a 2-8 whole number, and mis a 1-11 whole number; and the heterocyclic group is quinary or sexenary, and contains 1-2 heteroatoms selected from N, O and S. The invention also provides a preparation method of the nitrogen-atom-containing arteannuin dimers, a pharmaceutical composition of the nitrogen-atom-containing arteannuin dimers, and application of the nitrogen-atom-containing arteannuin dimers in preparing drugs for treating cancers, especially endometrial carcinoma, oophoroma, cervical carcinoma, breast cancer, colon cancer, lung cancer, prostatic cancer, liver cancer and/or stomach cancer.