Labeled inhibitors of prostate specific membrane antigen (PSMA), biological evaluation, and use as imaging agents

摘要

The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. Various 99mTc/Re-labeled compounds were prepared by attaching known Tc/Re chelating agents to an amino-functionalized PSMA inhibitor with or without a variable length linker moiety. Ex vivo biodistribution and in vivo imaging demonstrated the degree of specific binding to engineered PSMA+ PC3 PIP tumors.

主权项

1. A compound of formula II: Wherein AA1 is lysine and AA2 is glutamic acid; R′ is a substituted alkyl; R″ is a substituted alkyl; X and Z are each independently C1-C8 alkylene, which may be substituted with 0-5 RA; W is C(═O); Y is —NH—CO; RA, for each occurrence, is CO2H.