The invention discloses a 4-styryl pyridine compound with the structural formula (1), wherein the R1 is X or B, the X is hydrogen or chlorine or bromine, and the B is 2-methyl-2-alcohol-3-butyne alkynyl, the R2 is W or Y or Z, the W is hydrogen, the Y is tert-butoxy-formyl, the Z is benzoyl or formal cyclopropane and the n is 2 or 3. The 4-styryl pyridine compound has increment inhibitory activity to K562 cells and can be used for preparing antineoplastic agents.