The invention discloses 2-(3,4-dimethoxy)benzoyl-5-(4-substituted phenylethynyl)thiophene, whose structural formula is as follows: ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ; Its preparation method comprises steps: 1) In the presence of a catalyst, react 2-bromothiophene and 3,4-dimethoxybenzoyl chloride in a solvent, and subsequently purify and separate to obtain 2-(3,4-dimethoxy Methoxy) benzoyl-5-bromothiophene; 2) In the presence of tetrakis (triphenylphosphine) palladium, CuI, acid binding agent, 2-(3,4-dimethoxy) benzoyl- 5-bromothiophene and 4-substituted phenylacetylene are reacted in a solvent, followed by subsequent purification and separation. The application of the compound in the preparation of anti-mammary cancer targeted therapy drugs. The application of the compound in the preparation of an anti-breast cancer drug resistance reversal agent. The compound of the present invention has obvious anti-proliferation effect on human breast cancer cells and drug-resistant strains of breast cancer cells, and can be used to prepare anti-breast cancer targeted therapy drugs and anti-breast cancer drug resistance reversal agents. Moreover, the compound of the present invention has the potential for large-scale industrial production, and the cost is relatively low.