Synthesis, biological evaluation, and stability studies of raloxifene mono- and bis-sulfamates as dual-targeting agents

All three possible sulfamate derivatives of the selective estrogen receptor modulator Raloxifene (bis-sulfamate 7 and two mono-sulfamates 8–9) were synthesized and evaluated as inhibitors of the clinical drug target steroid sulfatase (STS), both in cell-free and in cell-based assays, and also as est...

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Bibliographic Details
Main Authors: Zaraei, S-O, Dohle, W, Anbar, HS, El-Gamal, R, Leblond, B, Foster, PA, Al-Tel, TH, Potter, BVL, El-Gamal, MI
Format: Journal article
Language:English
Published: Elsevier 2024