- Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for ERalpha.
Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for ERalpha.
Bioorganic & medicinal chemistry letters (2007-02-10)
Kevin D Dykstra, Liangqin Guo, Elizabeth T Birzin, Wanda Chan, Yi Tien Yang, Edward C Hayes, Carolyn A DaSilva, Lee-Yuh Pai, Ralph T Mosley, Bryan Kraker, Paula M D Fitzgerald, Frank DiNinno, Susan P Rohrer, James M Schaeffer, Milton L Hammond
PMID17289385
ABSTRACT
A novel class of indole ligands for estrogen receptor alpha have been discovered which exhibit potent affinity and high selectivity. Substitution of the bazedoxifene skeleton to the linker present in the HTS lead 1a provided 22b which was found to be 130-fold alpha-selective and acted as an antagonist of estradiol activity in uterine tissue and MCF-7 cancer cells.
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