Optimization of the alkyl side chain length of fluorine-18-labeled 7α-alkyl-fluoroestradiol
-
Add time:08/31/2019 Source:sciencedirect.com
IntroductionSeveral lines of evidence suggest that 7α-substituted estradiol derivatives bind to the estrogen receptor (ER). In line with this hypothesis, we designed and synthesized 18F-labeled 7α-fluoroalkylestradiol (Cn-7α-[18F]FES) derivatives as molecular probes for visualizing ERs. Previously, we successfully synthesized 7α-(3-[18F]fluoropropyl)estradiol (C3-7α-[18F]FES) and showed promising results for quantification of ER density in vivo, although extensive metabolism was observed in rodents. Therefore, optimization of the alkyl side chain length is needed to obtain suitable radioligands based on Cn-7α-substituted estradiol pharmacophores.
We also recommend Trading Suppliers and Manufacturers of (7α,17β)-3-Methoxy-7-Methyl-estra-1,3,5(10)-trien-17-ol (cas 15506-01-1). Pls Click Website Link as below: cas 15506-01-1 suppliers
Prev:Anti-tumor efficacy of new 7α-substituted androstanes as aromatase inhibitors in hormone-sensitive and resistant breast cancer cells
Next:Novel 7α-alkoxy-17α-(4′-halophenylethynyl)estradiols as potential SPECT/PET imaging agents for estrogen receptor expressing tumours: Synthesis and binding affinity evaluation) - 【Back】【Close 】【Print】【Add to favorite 】
- Related Information
- Anti-tumor efficacy of new 7α-substituted androstanes as aromatase inhibitors in hormone-sensitive and resistant breast cancer cells08/30/2019
- C-19-steroid 7α-hydroxylation by rat testes. isolation and identification of: 7α, 17β-dihydroxy-5α-androstan-3-one, 5α-androstan-3α,7α,17β-triol and 5α-androstane-3β,7α, 17β-triol08/29/2019
- A novel and stereoselective synthesis of 7α-alkynylestra-1,3,5(10)-triene-3,17β-estradiol08/28/2019
- Chemical synthesis and biochemical characterization of a biotinylated derivative of 17β-estradiol with a long side chain covalently attached to its C-7α position08/27/2019
- In vitro metabolism of dehydroepiandrosterone (DHEA) to 7α-hydroxy-DHEA and Δ5-androstene-3β,17β-diol in specific regions of the aging brain from Alzheimer’s and non-demented patients08/26/2019
- Original articleNew platinum(II) complexes conjugated at position 7α of 17β-acetyl-testosterone as new combi-molecules against prostate cancer: Design, synthesis, structure–activity relationships and biological evaluation08/25/2019
- 5α-Androstane-3β,7α,17β-triol and 5α-androstane-3β,7β,17β-triol as substrates for the human 11β-hydroxysteroid dehydrogenase type 108/24/2019
- Androst-5-ene-3β,7α/β,17β-triols, their plasma levels and dependence on the hypothalamic–pituitary–adrenal axis08/23/2019
