The invention relates to a novel derivatives of hyperpiperazine acetyl hydrazine class. The invention also relates to a method for the preparation of the hyperpiperazine acetyl hydrazine derivatives for use in the preparation of drugs for the treatment and/or prevention of cancer and/or cancer, comprising a pharmaceutical composition of the hyperpiperazine acetyl hydrazine derivatives. The hyperpiperazine acetyl hydrazine derivatives of the present invention have effective anti-tumor activity.