Title of article
Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for Erα
Author/Authors
Kevin D. Dykstra، نويسنده , , Liangqin Guo، نويسنده , , Elizabeth T. Birzin، نويسنده , , Wanda Chan، نويسنده , , Yi Tien Yang، نويسنده , , Edward C. Hayes، نويسنده , , Carolyn A. DaSilva، نويسنده , , Lee-Yuh Pai، نويسنده , , Ralph T. Mosley، نويسنده , , Bryan Kraker، نويسنده , , Paula M.D. Fitzgerald، نويسنده , , Frank DiNinno، نويسنده , , Susan P. Rohrer، نويسنده , , James M. Schaeffer، نويسنده , , Milton L. Hammond، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
7
From page
2322
To page
2328
Abstract
A novel class of indole ligands for estrogen receptor α 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 α-selective and acted as an antagonist of estradiol activity in uterine tissue and MCF-7 cancer cells.
Keywords
estrogen receptor , ER? , SERAMs , 2-Aryl indoles
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798035
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