Synthesis and Discovery of Estra-1,3,5(10),6,8-pentaene-2,16α-diol
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https://figshare.com/articles/dataset/Synthesis_and_Discovery_of_Estra-1_3_5_10_6_8-pentaene-2_16_-diol/7090916
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资源简介：
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.
创建时间：
2018-09-14
