Structure–Activity Relationship for the First??in??Class Clinical Steroid Sulfatase Inhibitor Irosustat (STX64, BN83495)

LW Woo, D Ganeshapillai, MP Thomas…

Index: Woo, L.W. Lawrence; Ganeshapillai, Dharshini; Thomas, Mark P.; Sutcliffe, Oliver B.; Malini, Bindu; Mahon, Mary F.; Purohit, Atul; Potter, Barry V.L. ChemMedChem, 2011 , vol. 6, # 11 p. 2019 - 2034

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Citation Number: 26

Abstract

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 ...