Center for Chemical Genetics, Institute of Molecular Genetics, vvi, Academy of Sciences of the Czech Republic, Prague, Czech Republic.
J Med Chem. 2010 May 27;53(10):4290-4. doi: 10.1021/jm901898a.
To identify novel estrogen receptor ligands a series of substituted 17alpha-arylestradiols were synthesized using the catalytic [2 + 2 + 2]cyclotrimerization of 17alpha-ethynylestradiol with various 1,7-diynes in the presence of Wilkinson's catalysts [Rh(PPh(3))(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 ERalpha/ERbeta and different selectivity as a result of differing potencies for either ER.
为了鉴定新的雌激素受体配体，我们使用炔雌醇与各种 1,7-二炔在 Wilkinson 催化剂 [Rh(PPh(3))(3)Cl]存在下的催化 [2 + 2 + 2]环三聚反应，合成了一系列取代的 17α-芳基雌二醇。这些化合物进行了竞争性结合测定、基于细胞的荧光素酶报告基因测定和增殖测定。这些实验证实了它们的雌激素特性，并揭示了一些有趣的性质，如 ERalpha/ERbeta 的混合部分/完全激动剂作用和由于 ER 效力的不同而导致的不同选择性。
