The invention discloses conjugates of beta-carboline-3-carboxylic acid and oligopeptides, preparation, a nano structure, and an application thereof as an antitumor agent. The invention discloses conjugates (8a-f) of beta-carboline-3-carboxylic acid and six oligopeptides, wherein the six oligopeptides are Leu-Pro-Asn-Ile-Ser-Lys-Pro (LPNISKP), Arg-Gly-Asp-Ser (RGDS), Arg-Gly-Asp-Phe (RGDF), Arg-Gly-Asp-Val (RGDV), Leu-Asp-Ser (LDV), and Lys-Glu (KE). The invention discloses a preparation method and nano structure of the conjugates, discloses an inhibition effect of the conjugates on five tumor cell strains namely HL60, HCT-8, HeLa, BEL-7402, and HepG2, and further discloses an inhibition effect on tumor growth of S180 tumor-bearing mice. The experiment results show that the provided conjugates of beta-carboline-3-carboxylic acid and six oligopeptides have an excellent antitumor effect, so that the conjugates is advantageous for being used as an antitumor drug in clinic.