| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1366842 | Bioorganic & Medicinal Chemistry Letters | 2007 | 7 Pages |
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.
Graphical abstractA 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.Figure optionsDownload full-size imageDownload as PowerPoint slide
