Abstract: The invention relates to novel camptothecin derivatives and their applications, tumor cell growth inhibitors, ternary complexes, and a method for improving the solubility of the camptothecin derivatives. The camptothecin derivatives are prepared by modifying the substance shown as Formula I with glycosylated triazole at position R3. In the structure shown as Formula I, R1 represents H, C1-10 alkyl, C1-10 alkyl-D or C1-10 haloalkyl; R2 represents H, CH2N(CH3)2 or CH2N(CD3)2; and R4 represents or H, wherein X represents N, O or S; and L represents polypeptide, C1-20 linear alkyl or derivatives thereof, C1-20 linear or branched acyl derivatives, C2-100 ethylene glycol or derivatives thereof. The camptothecin derivatives have high solubility, the anticancer drugs prepared from them have the advantages of wide anticancer spectrum and high safety, and have in vivo anticancer activity higher than irinotecan hydrochloride.