The invention belongs to the technical field of medicine, and relates to 2-[(pyridin-2-ylmethyl)thio]-1H-benzimidazole compounds and their preparation methods and applications. The general formula of described 2-[(pyridin-2-ylmethyl)thio]-1H-benzimidazoles and pharmaceutically acceptable salts is as follows: R 1 , R 2 Same or different, selected from hydrogen, C1‑C8 alkyl, C3‑C6 cycloalkyl, phenyl, halogen substituted phenyl, C1‑C4 alkyl substituted phenyl, C1‑C4 alkoxy substituted phenyl , phenyl substituted with halogen and C1‑C4 alkoxy, phenyl substituted with halogen and C1‑C4 alkoxy, phenyl substituted with halogen substituted C1‑C4 alkyl, benzyl, 4‑benzyloxy Phenyl; or R 1 , R 2 Together with the nitrogen atoms connected to them, they form substituted or unsubstituted morpholinyl, phenylpiperazine or benzhydrylpiperazine; the substituents are C1-C4 alkoxy, C1-C4 alkyl, halogen; R 3 , R 5 Can be selected from H, C1-C4 alkyl. The synthesis method of the compound of the invention is simple and convenient, suitable for industrial production, and has obvious antitumor activity.