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Journal of medicinal chemistry

2-Substituted 4-(thio) chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase

P Nussbaumer, P Lehr, A Billich

文献索引:Nussbaumer, Peter; Lehr, Philipp; Billich, Andreas Journal of Medicinal Chemistry, 2002 , vol. 45, # 19 p. 4310 - 4320

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被引用次数: 80

摘要

Steroid sulfatase (STS) has emerged as a highly attractive target for the therapy of a number of disorders. Starting with the known inhibitor estrone sulfamate (1) as lead compound and with the finding that steroid sulfamates containing a nonaromatic A-ring are inactive, chromen-4-one sulfamates were designed, prepared, and tested for their ability to block human STS. This new class of nonsteroidal inhibitors shows high potency when the ...