Design, synthesis and biochemical evaluation of aC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES)

We report the initial results of our study into a series of simple 4′-O-sulfamoyl-4-biphenyl based compounds as novel inhibitors of the enzyme estrone sulfatase (ES). The results of the study show that these compounds are potent inhibitors, possessing greater inhibitory activity than COUMATE, but weaker inhibitory activity than EMATE or the tricyclic derivative of COUMATE, namely 667-COUMATE. Furthermore, the compounds are observed to be irreversible inhibitors.