Estrogen receptor ligands. Part 9: Dihydrobenzoxathiin SERAMs with alkyl substituted pyrrolidine side chains and linkers.
Article Details
- CitationCopy to clipboard
Blizzard TA, Dininno F, Morgan JD 2nd, Chen HY, Wu JY, Kim S, Chan W, Birzin ET, Yang YT, Pai LY, Fitzgerald PM, Sharma N, Li Y, Zhang Z, Hayes EC, Dasilva CA, Tang W, Rohrer SP, Schaeffer JM, Hammond ML
Estrogen receptor ligands. Part 9: Dihydrobenzoxathiin SERAMs with alkyl substituted pyrrolidine side chains and linkers.
Bioorg Med Chem Lett. 2005 Jan 3;15(1):107-13.
- PubMed ID
- 15582421 [ View in PubMed]
- Abstract
A series of dihydrobenzoxathiin SERAMs with alkylated pyrrolidine side chains or alkylated linkers was prepared. Minor modifications in the side chain or linker resulted in significant effects on biological activity, especially in uterine tissue.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Compound 18 Estrogen receptor alpha IC 50 (nM) 1.7 N/A N/A Details Compound 4-D Estrogen receptor alpha IC 50 (nM) 0.8 N/A N/A Details Estradiol Estrogen receptor alpha IC 50 (nM) 1.3 N/A N/A Details Estradiol Estrogen receptor beta IC 50 (nM) 1.1 N/A N/A Details Raloxifene Estrogen receptor alpha IC 50 (nM) 1.8 N/A N/A Details Raloxifene Estrogen receptor beta IC 50 (nM) 12 N/A N/A Details