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• W2056192904 startingPage "2244" @default.
• W2056192904 abstract "Steroid sulfatase (STS) is a potential target for treatment of postmenopausal hormone-dependent breast cancer. Several steroidal STS inhibitors have been reported, but steroidal compounds are difficult to optimize and may interact with other targets. On the other hand, we have shown that diphenylmethane (DPM) derivatives act as estrogen receptor (ER) agonists and antagonists. Here, we aimed to design and synthesize non-steroidal DPM-type STS inhibitors that would also serve as pro-estrogen antagonists, releasing a metabolite with ERα-antagonistic activity upon hydrolysis by STS. We synthesized a series of compounds and evaluated their biological activities by means of STS-inhibitory activity assay and ER reporter gene assay. Among them, silicon-containing compound 16a showed strong STS-inhibitory activity (IC50 = 0.17 μM). Further, its putative metabolite (12a) exhibited potent ERα-antagonistic activity (IC50 = 29.7 nM)." @default.
• W2056192904 created "2016-06-24" @default.
• W2056192904 creator A5000147737 @default.
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• W2056192904 date "2014-04-01" @default.
• W2056192904 modified "2023-10-16" @default.
• W2056192904 title "Design and synthesis of silicon-containing steroid sulfatase inhibitors possessing pro-estrogen antagonistic character" @default.
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• W2056192904 doi "https://doi.org/10.1016/j.bmc.2014.02.025" @default.
• W2056192904 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/24630694" @default.
• W2056192904 hasPublicationYear "2014" @default.
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