Discovery of a sulfamate-based steroid sulfatase inhibitor with intrinsic selective estrogen receptor modulator properties
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- 作者：Charles Ouelleta ; René ; Maltaisa ; É ; tienne Ouelleta ; Xavier Barbeaub ; Patrick Lagü ; ec ; Donald Poiriera ; d ; donald.poirier@crchul.ulaval.ca" class="auth_mail" title="E-mail the corresponding author
- 关键词：Sulfatase ; Enzyme ; Inhibitor ; Estrogen ; Cancer ; SERM
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：25 August 2016
- 年：2016
- 卷：119
- 期：Complete
- 页码：169-182
- 全文大小：2683 K
文摘
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Tetrahydroisoquinoline derivatives were synthesized using an arylsulfamate linker.
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Sulfamate tetrahydroisoquinoline derivatives class="boldFont">32–class="boldFont">34 inhibit STS (IC50 = 3.9–16.6 nM).
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Sulfamate tetrahydroisoquinoline derivatives class="boldFont">32–class="boldFont">34 act as SERMs.
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Results are supported by molecular docking experiments.
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Sulfamate class="boldFont">33 represents a first sulfamate-based inhibitor with intrinsic SERM activity.