| Autor: |
Hanson RN; Department of Chemistry, Northeastern University, 360 Huntington Avenue, Boston, Massachusetts 02115-5000, USA. r.hanson@neu.edu, Friel CJ, Dilis R, Hughes A, DeSombre ER |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2005 Jun 30; Vol. 48 (13), pp. 4300-11. |
| DOI: |
10.1021/jm040157s |
| Abstrakt: |
As part of our ongoing program to develop probes for the hormone binding domain of the estrogen receptor-alpha (ERalpha), we prepared and evaluated a series of 17alpha,Z-(4-substituted-phenyl)vinyl estradiol derivatives. The results indicated that the relative binding affinities (RBAs) at 25 degrees C for the new compounds were significant (RBA = 9-57) although less than that of estradiol (RBA = 100) or of the parent unsubstituted phenylvinyl estradiol (RBA = 66). All of the Z-compounds were full agonists in the uterotrophic assay, indicating that the ligands formed estrogen-like complexes with the estrogen receptor-alpha hormone binding domain (ERalpha-HBD). Comparison of corresponding Z- and E-4-substituted phenylvinyl ligands complexed with the ERalpha-HBD indicated small but significant differences in binding modes that may account for the differing trends seen in the structure-activity relationships for the two series. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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