114031-67-3

Usage

Uses

Used in Organic Synthesis:
4-HYDROXY-4'-(TRIMETHYLACETOXY)BENZOPHENONE is used as an intermediate in the synthesis of various organic compounds. Its unique structure allows it to participate in a wide range of chemical reactions, making it a versatile building block for the creation of new molecules with diverse properties and applications.
Used in Pharmaceutical Industry:
In the pharmaceutical industry, 4-HYDROXY-4'-(TRIMETHYLACETOXY)BENZOPHENONE is used as a key component in the development of new drugs. Its ability to undergo various chemical transformations enables the creation of novel drug candidates with potential therapeutic benefits.
Used in Chemical Research:
4-HYDROXY-4'-(TRIMETHYLACETOXY)BENZOPHENONE is also utilized in chemical research as a model compound for studying reaction mechanisms and exploring new synthetic pathways. Its reactivity and structural features make it an ideal candidate for investigating various aspects of organic chemistry, including reaction kinetics, stereochemistry, and catalysis.
Used in Material Science:
In the field of material science, 4-HYDROXY-4'-(TRIMETHYLACETOXY)BENZOPHENONE can be employed in the development of new materials with specific properties. Its incorporation into polymers, for example, can lead to materials with enhanced thermal stability, mechanical strength, or optical properties, depending on the desired application.

Upstream product

• 611-99-4 4,4'-Dihydroxybenzophenone 
• 3282-30-2 pivaloyl chloride 
• 112004-83-8 [4-[4-(2,2-dimethylpropanoyloxy)benzoyl]phenyl] 2,2-dimethylpropanoate 
• 7065-46-5 3,3-dimethylbutanoic acid chloride 

Downstream Products

• 177748-18-4 2,2-Dimethyl-propionic acid 4-[(Z)-4-chloro-1-(4-hydroxy-phenyl)-2-phenyl-but-1-enyl]-phenyl ester 
• 177748-18-4 2,2-Dimethyl-propionic acid 4-[(E)-4-chloro-1-(4-hydroxy-phenyl)-2-phenyl-but-1-enyl]-phenyl ester 
• 177748-17-3 2,2-Dimethyl-propionic acid 4-[(Z)-1-(4-hydroxy-phenyl)-2-phenyl-but-1-enyl]-phenyl ester 
• 177748-17-3 (E)-1-(4-hydroxyphenyl)-1-[4-(trimethylacetoxy)phenyl]-2-phenylbut-1-ene 
• 364635-60-9 1-(4-trimethylacetoxyphenyl)-1-(p-hydroxyphenyl)-2-phenylbut-1-ene 
• 177748-18-4 2,2-Dimethyl-propionic acid 4-[(E)-4-chloro-1-(4-hydroxy-phenyl)-2-phenyl-but-1-enyl]-phenyl ester 
• 1133415-48-1 1-(4-hydroxyphenyl)-1,2-bis(4-trimethylacetoxyphenyl)but-1-ene 
• 1440533-08-3 (Z)-4-(1-(4-(2-amino-2-oxoethoxy)phenyl)-2-phenylbut-1-enyl)phenyl Pivalate 
• 1308808-22-1 (Z)-4-(1-(4-(2-aminoethoxy)phenyl)-2-phenylbut-1-enyl)phenol 
• 1440533-06-1 (E)-4-(1-(4-(2-amino-2-oxoethoxy)phenyl)-2-phenylbut-1-enyl)phenyl Pivalate 
• 119757-57-2 (E,Z)-1-<4-(2-chloroethoxy)phenyl>-1-(4-hydroxyphenyl)-2-phenyl-1-butene 

Relevant academic research and scientific papers

Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRγ

The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are described. The binding affinities of these compounds toward the orphan estrogen-related receptor γ and the classical estrogen receptor α demonstrate that analogs bearing hydroxyalkyl g

A multi-gram-scale stereoselective synthesis of Z-endoxifen

Z-Endoxifen is widely regarded as the most active metabolite of tamoxifen, and has recently demonstrated a 26.3% clinical benefit in a phase I clinical trial to treat metastatic breast cancer after the failure of standard endocrine therapy. Future pharmac

Rational design of ERα targeting hypoxia turn-on fluorescent probes with antiproliferative activity for breast cancer

The overexpression of estrogen receptor (ER) α is not only closely related to the development of ER+ breast cancer, but is also an important biomarker for clinical diagnosis and treatment. Herein, we report several ERα targeting hypoxia turn-on fluorescent probes with antitumor activity for breast cancer cells. Among them, probes 3 and 5 displayed good ERα targeting ability and favorable hypoxia turn-on response in MCF-7 cells. Moreover, the probes 3 and 5 exhibited good antiproliferative activity towards MCF-7 cells (IC50 = 8.5 μM, 10.3 μM) and a much lower cytotoxicity to normal cells compared with the positive control. It is expected that these novel fluorescent probes may provide useful tools for the theranostics of ER+ breast cancer.

NOVEL COMPOUNDS HAVING ESTROGEN RECEPTOR ALPHA DEGRADATION ACTIVITY AND USES THEREOF

The present disclosure relates to novel compounds having estrogen receptor alpha degradation activity, pharmaceutical compositions containing such compounds, and their use in prevention and treatment of cancer and related diseases and conditions.

NOVEL ARYL ETHANE DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT

The present invention relates to an aryl ethene derivative, for inhibiting an estrogen-related receptor gamma (ERRγ) activity, a prodrug of same, a solvate of same, a stereoisomer of same or pharmaceutically acceptable salts of same, and a pharmaceutical

ANTI-CANCER NUCLEAR HORMONE RECEPTOR-TARGETING COMPOUNDS

The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.

NOVEL ARYL ETHENE DERIVATIVES AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME AS AN ACTIVE INGREDIENT

The present invention relates to an aryl ethene derivative represented by chemical formula 1 which suppresses the activity of estrogen-related receptor gamma (ERRandgamma;), a prodrug thereof, a solvate thereof, a stereomer thereof, or a pharmaceutically acceptable salt thereof, and to a pharmaceutical composition comprising the same as an effective component. In the chemical formula 1, R^1, R^2, L and Ar are the same as defined in the detailed description of the invention.COPYRIGHT KIPO 2018

Synthesis and biological evaluation of novel 4-hydroxytamoxifen analogs as estrogen-related receptor gamma inverse agonists

Estrogen-related receptor gamma (ERRγ) has recently been recognized as an attractive target for treating inflammation, cancer, and metabolic disorders. Herein, we discovered and demonstrated the in vitro pharmacology as well as the absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties of chemical entities that could act as highly selective inverse agonists for ERRγ. The results were comparable to those for GSK5182 (4), a leading ERRγ inverse agonist ligand. Briefly, the half-maximal inhibitory concentration (IC50) range of the synthesized compounds for ERRγ was 0.1-10 μM. Impressively, compound 24e exhibited potency comparable to 4 but was more selective for ERRγ over three other subtypes: ERRα, ERRβ, and estrogen receptor α. Furthermore, compound 24e exhibited a superior in vitro ADMET profile compared to the other compounds. Thus, the newly synthesized class of ERRγ inverse agonists could be lead candidates for developing clinical therapies for ERRγ-related disorders.

Utilization of the inherent nucleophile for regioselective O-acylation of polyphenols via an intermolecular cooperative transesterification

A green and efficient method for regioselective O-acylation of polyphenols has been developed. The acylation can be carried out in potassium carbonate/dimethyl sulphoxide system by utilizing the ‘inherent nucleophile’ via an intermolecular cooperative transesterification under mild condition. This method shows particular advantage in regioselective acylation of polyphenols bearing 2′,4′-dihydroxyacetophenone moiety and can be extended to the synthesis of mono or multiple acetates of polyphenols without this moiety in good yields. Compared with other reported approaches, this method is endowed with atom economy and is more environment-friendly for avoiding the use of any metal-based catalysts.

Synthesis of mixed (E, Z)-, (E)-, and (Z)-norendoxifen with dual aromatase inhibitory and estrogen receptor modulatory activities

The first synthesis of the tamoxifen metabolite norendoxifen is reported. This included syntheses of (E)-norendoxifen, (Z)-norendoxifen, and (E,Z)-norendoxifen isomers. (Z)-Norendoxifen displayed affinity for aromatase (Ki 442 nM), estrogen receptor-α (EC50 17 nM), and estrogen receptor-β (EC50 27.5 nM), while the corresponding values for (E)-norendoxifen were aromatase (Ki 48 nM), estrogen receptor-α (EC50 58.7 nM), and estrogen receptor-β (EC50 78.5 nM). Docking and energy minimization studies were performed with (E)-norendoxifen on aromatase, and the results provide a foundation for structure-based drug design. The oral pharmacokinetic parameters for (E,Z)-norendoxifen were determined in mice, and (Z)-norendoxifen was found to result in significantly higher plasma concentrations and exposures (AUC values) than (E)-norendoxifen. The affinities of both isomers for aromatase and the estrogen receptors, as well as the pharmacokinetic results, support the further development of norendoxifen and its analogues for breast cancer treatment.