Compounds of the formula, A-L-B, wherein A is glutamate or a glutamate analog； L is a phosphoramidate or a phosphoramidate analog； and B is serine or a serine analog are described which are potent inhibitors of prostate-specific membrane antigen (PMSA). Such compounds are useful in treatment of prostate cancer； and when chemically attached to a fluorescent dye, can efficiently and selectively label prostate cancer cells for fluorescent imaging.
