| Name | estrogen receptor |
|---|---|
| Synonyms | ER; ERA; ER alpha; ERalpha; ESR; ESR 1; ESR1; ESRA… |
| Name | naphthalene |
|---|---|
| CAS | naphthalene |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 18722117 | Fang J, Akwabi-Ameyaw A, Britton JE, Katamreddy SR, Navas F 3rd, Miller AB, Williams SP, Gray DW, Orband-Miller LA, Shearin J, Heyer D: Synthesis of 3-alkyl naphthalenes as novel estrogen receptor ligands. . Bioorg Med Chem Lett. 2008 Sep 15;18(18):5075-7. Epub 2008 Aug 5. A series of estrogen receptor ligands based on a 3-alkyl naphthalene scaffold was synthesized using an intramolecular enolate-alkyne cycloaromatization as the key step. |
83(1,1,1,3) | Details |
| 16845439 | Gennari L: Lasofoxifene: a new type of selective estrogen receptor modulator for the treatment of osteoporosis. Drugs Today. 2006 Jun;42(6):355-67. Lasofoxifene (CP 336,156) is a naphthalene-derivative, third-generation SERM, structurally distinct from the first- and second-generation SERMs. |
3(0,0,0,3) | Details |
| 18324762 | Frotscher M, Ziegler E, Marchais-Oberwinkler S, Kruchten P, Neugebauer A, Fetzer L, Scherer C, Muller-Vieira U, Messinger J, Thole H, Hartmann RW: Design, synthesis, and biological evaluation of (hydroxyphenyl) naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of -dependent diseases. J Med Chem. 2008 Apr 10;51(7):2158-69. Epub 2008 Mar 7. This reaction takes place in the target cell where the estrogenic effect is exerted via the estrogen receptor (ER). |
2(0,0,0,2) | Details |
| 19303142 | Passos AL, Pinto PI, Power DM, Canario AV: A yeast assay based on the gilthead sea bream (teleost fish) estrogen receptor beta for monitoring mimics. Ecotoxicol Environ Saf. 2009 Jul;72(5):1529-37. Epub 2009 Mar 19. The induction of beta-galactosidase activity was strictly dependent on the presence of seabream (Sparus aurata) betaa estrogen receptor (sbERbetaa) and substances known to have estrogenic activity. 17beta- (E (2)) and diethylstilbestrol (DES), both agonists, were most active and the antagonist tamoxifen (TAM) was 14-fold less active than E (2). Among the chemicals tested bisphenol-A was most active, followed by pentachlorophenol and naphthalene. |
1(0,0,0,1) | Details |
| 16428131 | Asikainen AH, Ruuskanen J, Tuppurainen KA: Alternative QSAR models for selected and cytochrome P450 ligands: comparison between classical, spectroscopic, CoMFA and GRID/GOLPE methods. SAR QSAR Environ Res. 2005 Dec;16(6):555-65. The performance of the spectroscopic EVA (eigenvalue) and EEVA (electronic eigenvalue) methods was tested with data sets applying 7-hydroxylation inhibitors (28 compounds) for cytochrome P450 mouse CYP2A5 and human CYP2A6 enzymes and 11ss-, 16a-, and 17a-substituted derivatives (30 compounds) for the lamb uterine estrogen receptor, and compared with the performance of the classical Hansch-type, CoMFA and GRID/GOLPE methods. |
1(0,0,0,1) | Details |
| 18950679 | Marchais-Oberwinkler S, Frotscher M, Ziegler E, Werth R, Kruchten P, Messinger J, Thole H, Hartmann RW: Structure-activity study in the class of 6-(3'-hydroxyphenyl) naphthalenes leading to an optimization of a pharmacophore model for 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitors. Mol Cell Endocrinol. 2009 Mar 25;301(1-2):205-11. Epub 2008 Oct 4. After identification of the 6-(3'-hydroxyphenyl)-2-naphthol scaffold 1, the potency of this class of inhibitors was further improved by substitution of the 1-position of the naphthalene ring by a phenyl group (compound 18, IC (50)=20nM). Compound 18 also showed a good selectivity toward 17beta-HSD2 and the estrogen receptors alpha and beta. |
1(0,0,0,1) | Details |