Steroids

Structure-activity relationship studies of the amide functionality in (pO-sulfamoyl)-N-alkanoyl tyramines as estrone sulfatase inhibitors

…, S Milano, L Kluth, M Rhodes, R Boni, DA Johnson…

Index: Chu, Guo-Hua; Milano, Shawn; Kluth, Lisa; Rhodes, Michael; Boni, Riccardo; Johnson, David A.; Li, Pui-Kai Steroids, 1997 , vol. 62, # 7 p. 530 - 535

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Citation Number: 21

Abstract

Recently, we reported the synthesis and biochemical studies of a series of (pO-sulfamoyl)-N- alkanoyl tyramines as nonsteroidal estrone sulfatase inhibitors. One of the most potent inhibitors in this series is (pO-sulfamoyl)-N-tridecanoyl tyramine 1 with an IC50 value of 61.3 nM. In this study, we synthesized four analogs of 1 (compounds 2–5) to investigate the structure-activity relationships of the amide functionality in (pO-sulfamoyl)-N-tridecanoyl ...