Phosphonates and thiophosphonates as sulfate surrogates: synthesis of estrone 3-methylthiophosphonate, a potent inhibitor of estrone sulfatase

Estrone 3-phosphonaters and thiophosphonates have been synthesised as analogues of estrone 3-sulfate and exhibit potent activity as competitive inhibitors of estrone sulfatase, a potential therapeutic target in treatment of breast cancer. Estrone 3-methylthiophosphonate is a potent inhibitor of estr...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1993-02, Vol.3 (2), p.313-318
Main Authors: Howarth, Nicola M, Cooper, Gary, Purohit, Atul, Duncan, Lorna, Reed, Michael J, Potter, Barry VL
Format: Article
Language:English
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Summary:Estrone 3-phosphonaters and thiophosphonates have been synthesised as analogues of estrone 3-sulfate and exhibit potent activity as competitive inhibitors of estrone sulfatase, a potential therapeutic target in treatment of breast cancer. Estrone 3-methylthiophosphonate is a potent inhibitor of estrone sulfatase.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)80900-8