This invention provides a ligand compound and chelate for targeting PSMA, and their applications. The
structural formula of the compound is shown in Formula I-1, wherein X is -(CH2). m -CONH-CHR3(CH2) n -R4, R3 are selected from
hydrogen, C1-C5 straight-chain or branched
alkyl, C1-C5 straight-chain or branched alkoxy, C1-C5 straight-chain or branched alkylthio,
halogen, cyano, nitro, hydroxy, carboxyl,
sulfonic acid, phenyl, and amino-substituted C1-C5 straight-chain or branched
alkyl; R4 is selected from optionally substituted C1-C5 straight-chain or branched
alkyl, optionally substituted C1-C5 straight-chain or branched alkoxy, optionally substituted C1-C5 straight-chain or branched alkylthio, optionally substituted 6-14
aryl, optionally substituted 5-14 heteroaryl, as well as
halogen, cyano, nitro, hydroxy, carboxyl,
sulfonic acid, C1-C5 straight-chain or branched alkylamide and C1-C5 straight-chain or branched alkylsulfonamide; m is an integer from 2 to 4; n is an integer from 1 to 3; Z is a radioactive
metal ion chelating group. The stability and safety of this PSMA-targeting ligand compound were significantly improved, and it exhibited superior tumor-suppressive effects.