Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for ERalpha

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 antagoni...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 17; no. 8; p. 2322
Main Authors Dykstra, Kevin D, Guo, Liangqin, Birzin, Elizabeth T, Chan, Wanda, Yang, Yi Tien, Hayes, Edward C, DaSilva, Carolyn A, Pai, Lee-Yuh, Mosley, Ralph T, Kraker, Bryan, Fitzgerald, Paula M D, DiNinno, Frank, Rohrer, Susan P, Schaeffer, James M, Hammond, Milton L
Format Journal Article
LanguageEnglish
Published England 15.04.2007
Subjects
Breast Neoplasms - drug therapy
Cell Line, Tumor
Estrogen Antagonists - chemistry
Estrogen Antagonists - pharmacology
Estrogen Receptor alpha - antagonists & inhibitors
Female
Humans
Indoles - chemistry
Indoles - pharmacokinetics
Inhibitory Concentration 50
Ligands
Uterus - drug effects
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Summary: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.
ISSN:0960-894X