Disclosed are a difluoromethoxy diphenylethane and trans-stilbene derivatives, and a preparation method therefor and the use thereof. The present invention conducts a chemical structure modification with a difluoromethoxy group at the 4' position of the B-aryl ring of diphenylethane/stilbene, and the 3' position thereof is modified into a substituent such as a nitro, amino or hydroxyl. The difluoromethoxy diphenylethane and trans-stilbene derivatives obtained by the present invention have strong anti-tumour activity in vitro, with the introduction of the difluoromethyl changing the physical, chemical and biological properties of the compounds, and have a significant inhibitory effect on tumour cells.