Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans.
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Liu J, Birzin ET, Chan W, Yang YT, Pai LY, Dasilva C, Hayes EC, Mosley RT, Dininno F, Rohrer SP, Schaeffer JM, Hammond ML
Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans.
Bioorg Med Chem Lett. 2005 Feb 1;15(3):715-8.
- PubMed ID
- 15664843 [ View in PubMed]
- Abstract
The ring oxygen and sulfur analogs of lasofoxifene, 1a and 1b, were synthesized in an attempt to impart ERalpha selectivity, as found in the closely related dihydrobenzoxathiin compound I, recently discovered in these laboratories. The resulting isochroman and isothiochroman compounds were found to exhibit equipotent binding affinities to the ER isoforms and were less active in the inhibition of estradiol-triggered uterine growth when compared to I and lasofoxifene.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) 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