41164-36-7

Usage

InChI:InChI=1/C20H26O4/c1-20-9-8-15-14-5-3-13(24-11-19(22)23)10-12(14)2-4-16(15)17(20)6-7-18(20)21/h3,5,10,15-18,21H,2,4,6-9,11H2,1H3,(H,22,23)/t15-,16-,17+,18+,20+/m1/s1

Upstream product

• 41164-35-6 ethyl 2-{[(17β)-17-hydroxyestra-1,3,5(10)-trien-3-yl]oxy}acetate 
• 1428-66-6 2-(((8R,9S,13S,14S)-13-methyl-17-oxo-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-yl)oxy)acetic acid 
• 1350306-67-0 C₂₄H₃₂O₅ 
• 1743-60-8 17-β-estradiol 17-acetate 
• 50-28-2 estradiol 
• 139116-04-4 ((8R,9S,13S,14S,17S)-17-Hydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-yloxy)-acetic acid benzyl ester 
• 79-08-3 bromoacetic acid 
• 105-39-5 chloroacetic acid ethyl ester 
• 64-17-5 ethanol 
• 141-52-6 sodium ethanolate 

Downstream Products

• 946144-06-5 estradiol-3-O-acetyl-Arg(Nω-NO2)-Gly-Asp(OBn)-Ser(Bn)-OBn 
• 906673-90-3 estradiol-3-O-acetyl-Arg(Nω-NO2)-Gly-Asp(OBn)-Val-OBn 
• 906673-91-4 estradiol-3-O-acetyl-Arg(Nω-NO2)-Gly-Asp(OBn)-Phe-OBn 
• 1082573-01-0 C₃₃H₄₈N₂O₄ 
• 1147834-64-7 estradiol-3-O-acetyl-Arg(Nω-NO2)-Gly-Asp(OBn)-Phe-Arg(Nω-NO2)-Gly-Asp(OBn)-Phe-OBn 
• 1147834-62-5 estradiol-3-O-acetyl-Arg(Nω-NO2)-Gly-Asp(OBn)-Val-Arg(Nω-NO2)-Gly-Asp(OBn)-Val-OBn 
• 1147834-60-3 estradiol-3-O-acetyl-Arg(Nω-NO2)-Gly-Asp(OBn)-Ser(Bn)-Arg(Nω-NO2)-Gly-Asp(OBn)-Ser(Bn)-OBn 

Relevant academic research and scientific papers

Homogeneous enzyme immunoassay of estradiol using estradiol-3-O-carboxymethyl ether as hapten

A homogeneous enzyme immunoassay for estradiol estimation has been developed, which can be extended to other steroids. A new procedure for the preparation of estradiol -3-0- carboxymethyl ether by a simple one step reaction in high yield (90%) has been described. This hapten has been used for raising highly specific anti-estradiol antibody in rabbits and for preparation of enzyme conjugates. Two different enzymes, lysozyme and glucose -6- phosphate dehydrogenase have been studied for their suitability as enzyme labels. Our results indicate that lysozyme-conjugate meets the essential requirement for a practical enzyme immunoassay. The advantage of the present non-radioactive procedure is the overall simplicity, low cost and high stability of the reagents.

2-Methoxydiol derivatives as new tubulin and HDAC dual-targeting inhibitors, displaying antitumor and antiangiogenic response

Multi-target drugs design has become an active research field because of their advantages in cancer treatment. In present study, HDAC inhibitors pharmacophore and 2-methoxyestradiol(2ME2) were combined into a new hybrid molecule for the first t

N omega-Asp-N alpha-(17 beta-estradiol-3-acetyl)-Lys, as well as preparation, activity and application thereof

The invention discloses N omega-Asp-N alpha-(17 beta-estradiol-3-acetyl)-Lys having the formula in the specification, a preparation method thereof, a stepwise stability constant of the N omega-Asp-N alpha-(17 beta-estradiol-3-acetyl)-Lys complexed with Ca

1-asparaginic acid conjugate-3-estrone and preparation, nano structure, anti-osteoporosis activity and application thereof

The invention discloses 1-molecule asparaginic acid conjugate 3-molecule estradiol compound (called 1-asparaginic acid conjugate-3-estrone for short) which is shown in a following formula, discloses apreparation thereof, discloses a nano structure thereof and further discloses an anti-osteoporosis effect thereof on a chemical-castration female mouse osteoporosis model. Therefore, the invention discloses an application prospect thereof in preparing anti-osteoporosis medicine. The formula is shown in the description.

Glucagon superfamily peptides exhibiting nuclear hormone receptor activity

Provided herein are glucagon superfamily peptides conjugated with NHR ligands that are capable of acting at a nuclear hormone receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided here

GLUCAGON SUPERFAMILY PEPTIDES EXHIBITING GLUCOCORTICOID RECEPTOR ACTIVITY

Provided herein are glucagon superfamily peptides conjugated with GR ligands that are capable of acting at a glucocorticoid receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided herein

Immunosensors for estradiol and ethinylestradiol based on new synthetic estrogen derivatives: Application to wastewater analysis

Novel electrochemical immunosensors for sensitive detection of 17-β estradiol (E2) and ethinylestradiol (EE2) are described on the basis of the use of magnetic beads (MBs) as solid support and screen-printed electrodes as sensing platforms. Four synthetic estrogen derivatives containing either a carboxylic group or an amine group at the C-3 position were synthesized and covalently bound to MBs functionalized with amine or carboxyl groups, respectively. The assay was based on competition between the free and immobilized estrogen for the binding sites of the primary antibody, with subsequent revelation using alkaline phosphatase-labeled secondary antibody. Preliminary colorimetric tests were performed in order to validate the applicability of the synthetic estrogens to immuno-recognition and to optimize different experimental parameters. In a second step, electrochemical detection was carried out by square wave voltammetry (SWV). Under the optimized working conditions, the electrochemical immunosensors showed a highly sensitive response to E2 and EE2, with respective detection limits of 1 and 10 ng/L. Cross-reactivity evaluated against other hormones demonstrated an excellent selectivity. The developed devices were successfully applied to analysis of spiked and natural water samples. These new immunosensors offer the advantages of being highly sensitive, easy, and rapid to prepare, with a short assay time.

Oxidation of organic molecules in homogeneous aqueous solution catalyzed by hybrid biocatalysts (based on the Trojan Horse strategy)

New anionic metalloporphyrin-estradiol conjugates have been synthesized and fully characterized, and have been further associated to a monoclonal anti-estradiol antibody 7A3, to generate new artificial metalloenzymes following the so-called [Trojan Horse] strategy. The spectroscopic characteristics and dissociation constants of these complexes were similar to those obtained for the artificial metalloproteins obtained by association of cationic metalloporphyrin-estradiol conjugates to 7A3. This demonstrates that the nature of the porphyrin substituents, anionic or cationic, had little influence on the association with the antibody that is mainly driven by the tight association of the estradiol anchor with the binding pocket of the antibody. These new biocatalysts appeared to have an interesting catalytic activity in oxidation reactions. The iron(III)-anionic-porphyrin-estradiol-antibody complexes were found able to catalyze the chemoselective and slightly enantioselective (ee = 10%) sulfoxidation of sulfides by H2O2. The Mn(III)-porphyrin-estradiol-antibody complexes were found to catalyze the oxidation of styrene by KHSO5, the Mn(III)-cationic-porphyrin- estradiol-antibody complexes even showing the highest yields so far reported for the oxidation of styrene catalyzed by artificial metalloproteins. However, a lack of chemoselectivity and enantioselectivity was observed, which was probably due to a weak interaction of the metalloporphyrin cofactor with the binding pocket of antibody 7A3, as suggested by the similar UV-visible characteristics and catalytic activities obtained with both anionic and cationic porphyrins.

Synthesis, evaluation and 3D QSAR analysis of novel estradiol-RGD octapeptide conjugates with oral anti-osteoporosis activity

To enhance the potency, reduce the side effects and improve oral property of estradiol in estrogen replacement therapy (ERT), 6 novel estradiol-RGD octapeptide conjugates have been prepared. In an ovariectomized mouse osteoporotic model, at an oral dosage

3D QSAR of novel estrogen-RGD peptide conjugates: Getting insight into structural dependence of anti-osteoporosis activity and side effect of estrogen in ERT

To explore the structural dependence of the oral potency and side effect of estrogen-RGD peptide conjugates, here six novel conjugates were prepared via introducing RGD-tetrapeptides into both 3- and 17-positions of estradiol, and introducing RGD-octapept