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- W2891452960 abstract "A metallacycle-centered approach to the assembly of partially aromatic synthetic steroids was investigated as a means to prepare a boutique collection of unique steroidal agents. The synthesis and discovery of estra-1,3,5(10),6,8-pentaene-2,16α-diol (VII) is described, along with structure–activity relationships related to its cytotoxic properties. Overall, VII was found to have a GI50 = 0.2 μg/mL (∼800 nM) in MDA-MB-231 human breast cancer cells, be an efficacious estrogen receptor agonist with potency for ERβ > ERα (ERβ EC50 = 21 nM), possess selective affinity to the cdc-2-like kinase CLK4 (Kd = 350 nM), and be phenotypically related to paclitaxel by an unbiased panel assessment." @default.
- W2891452960 created "2018-09-27" @default.
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- W2891452960 date "2018-09-17" @default.
- W2891452960 modified "2023-10-16" @default.
- W2891452960 title "Synthesis and Discovery of Estra-1,3,5(10),6,8-pentaene-2,16α-diol" @default.
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- W2891452960 doi "https://doi.org/10.1021/acs.orglett.8b02689" @default.
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