期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 53, 期 10, 页码 4290-4294出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm901898a
关键词
-
资金
- Ministry of Education, Youth and Sports of the Czech Republic [LC06077]
- [AV0Z50520514]
- [Z40550506]
- [MSM0021620857]
To identify novel estrogen receptor ligands a series of substituted 17 alpha-arylestradiols were synthesized using the catalytic [2 + 2 + 2]cyclotrimerization of 17 alpha-ethynylestradiol with various 1,7-diynes in the presence of Wilkinson's catalysts [Rh(PPH3)(3)Cl]. The compounds were subjected to competitive binding assays, cell-based luciferase reporter assays, and proliferation assays. These experiments confirmed their estrogenic character and revealed some interesting properties like mixed partial/full agonism for ER alpha/ ER beta and different selectivity as a result of differing potencies for either ER.
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