The invention provides a farnesyl thiosalicylic acid-nucleoside conjugate and pharmaceutically acceptable salts thereof. The farnesyl thiosalicylic acid-nucleoside conjugate and the pharmaceutically acceptable salts thereof have the structure as shown in a general formula I, wherein in the general formula I, X is H, F, Cl or Br; R1 represents H, OH, OAc, SH, -OP(O)(OH)2, -OPO3HNa, -OP(O)(ONA)2, -OPO3HK or -OP(O)(OK)2; R2 represents H, OH, OAc or OCH; R3 represents H, OH, F, CN, OAc or OCH3; R4 represents H, OH, F, CN, OAc or OCH3. The invention also provides a preparation method of the farnesyl thiosalicylic acid-nucleoside conjugate and the pharmaceutically acceptable salts thereof and a pharmaceutical composition containing the derivatives as well as medical applications thereof, especially application in preparation of antitumor drug medicines.