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• W2764104203 abstract "The female hormone 17 β-estradiol (E2) is synthesized from estrone by steroid sulfatase (STS), and metabolized into 2-methoxyestradiol (2-ME), whereby the biological activity of the latter is substantially different from that of E2. Based on the metabolic pathways of E2, a carborane-containing 2-ME mimic (1c) and its derivatives (1 and 2) were designed and synthesized as novel multitarget anticancer agents. Bissulfamate 1f exhibited potent STS-inhibitory activity and tubulin-polymerization-inhibitory activity. Moreover, the cell-growth-inhibitory (CGI) activity of 1f was similar to that of 2-ME in a panel screening against 39 human cancer cell lines. Accordingly, 1f should be a promising perspective therapeutic agent for hormone-dependent breast tissue." @default.
• W2764104203 created "2017-10-20" @default.
• W2764104203 creator A5028510511 @default.
• W2764104203 creator A5033844318 @default.
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• W2764104203 date "2017-12-01" @default.
• W2764104203 modified "2023-10-17" @default.
• W2764104203 title "Novel p-carborane-containing multitarget anticancer agents inspired by the metabolism of 17β-estradiol" @default.
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• W2764104203 doi "https://doi.org/10.1016/j.bmc.2017.10.006" @default.
• W2764104203 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/29054710" @default.
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