Abstract Structure–activity relationship studies were conducted on Irosustat (STX64, BN83495), the first steroid sulfatase (STS) inhibitor to enter diverse clinical trials for patients with advanced hormone-dependent cancer. The size of its aliphatic ring was expanded; its sulfamate group was N, N-dimethylated, relocated to another position and flanked by an adjacent methoxy group; and series of quinolin-2 (1H)-one and quinoline derivatives of ...
