The present disclosure relates to a
gramine-
platinum(IV) complex as well as a preparation method therefor and the anti-tumor use thereof. One
gramine molecule is introduced to one side of the axial direction of a
platinum(IV) coordination center to form a mono-substituted tetravalent
platinum complex; or one
gramine molecule is introduced to one side of the axial direction of the platinum(IV) coordination center, and one molecule of a -NH-aliphatic chain group or an aliphatic chain group is introduced to the other side so as to form a bi-substituted tetravalent
platinum complex. The prepared complex has stronger killing ability on
tumor cells, and has obviously improved antiproliferative activity in various
cell lines; and in triple-negative
breast cancer cells having an extremely high malignant degree, the complex compared with clinical platinum drugs has most remarkable effect improvement. The gramine-platinum(IV) complex of the present disclosure has a simple synthesis process and low cost; said complex greatly improves the
curative effect of combined
drug therapy; and compared with traditional
divalent platinum and similar tetravalent platinum drugs, said complex has the advantages of good
curative effect, small
side effect and the like.