132589-92-5

Upstream product

• 5720-07-0 4-methoxyphenylboronic acid 
• 52381-02-9 3,4-bis(4-methoxyphenyl)furan 
• 104-01-8 4-Methoxyphenylacetic acid 
• 2632-13-5 2-Bromo-4'-methoxyacetophenone 
• 42766-36-9 potassium p-methoxyphenylacetate 
• 132589-78-7 2-(4-methoxyphenyl)-2-carbonylethyl-2-(4-methoxyphenyl)acetate 
• 132589-84-5 3,4-di(4-methoxyphenyl)-2,5-dihydrofuran-2-one 
• 132589-88-9 3,4-bis(4-hydroxyphenyl)-2H,5H-furan-2-one 
• 100-06-1 1-(4-methoxyphenyl)ethanone 

Relevant academic research and scientific papers

Oxygen bridge bicyclo - [2.2.1] - heptene compounds containing different covalent bullet structures, and preparation and application thereof

The invention discloses an oxygen bridge bicyclo - [2.2.1] - heptene compound containing different covalent popping structures as well as preparation and application thereof, and belongs to the technical field of targeted drugs. As shown in general formula (I) or general formula (II), furan derivatives and vinylsulfonamide derivatives or vinylsulfonate derivatives containing different covalent popping heads are prepared by reacting Diels-Alder to obtain a compound of the present invention. The compound can be used for preparing anti-breast cancer drugs. A medicament for the degradation of estrogen receptors, a medicament for a mutant estrogen receptor. Compared with the existing anti-breast cancer drug tamoxifen, MCF-7 cells have stronger inhibitory activity and have the ability to down-regulate the estrogen receptor level, and the activity shown for the mutant estrogen receptor is 4 - times of 5-10 hydroxytamoxifen.

Selective estrogen receptor modulator compounds containing phenylselenyl and application of compounds in anti-breast cancer drugs

The present invention discloses selective estrogen receptor modulator compounds containing phenylselenyl and an application of the compounds in anti-breast cancer drugs. According to the compounds provided by the present invention, 3-(4-hydroxyphenyl)-4-(

Oxo-bridged bicyclo-heptylene sulfonamides compound containing different alkyl chain lengths, as well as preparation method and application thereof

The invention discloses an oxo-bridged bicyclo-heptylene sulfonamides compound containing different alkyl chain lengths, as well as a preparation method and application thereof, and belongs to the technical field of medicines. 3-(4-hydroxycyclohexyl pheny

Oxygen bridge bis-heptylene sulfonamide compound containing suberic acid monoanilide group as well as synthesizing method, application and anti-breast cancer drug composition of oxygen bridge bis-heptylene sulfonamide compound

The invention belongs to technical field of medicines and specifically relates to an oxygen bridge bis-heptylene sulfonamide compound containing a suberic acid monoanilide group as well as a synthesizing method, application and an anti-breast cancer drug composition of the oxygen bridge bis-heptylene sulfonamide compound. The oxygen bridge bis-heptylene sulfonamide compound containing the suberic acid monoanilide group is prepared by one-step reaction of the following raw materials: 3-(4-hydroxyphenyl)-4-suberic acid monoanilino-furan and an ethenyl sulfonamide derivative at the temperature of 90 DEG C for 3 without a solvent or a catalyst. The oxygen bridge bis-heptylene sulfonamide compound is different from the existing anti-breast cancer drug tamoxifen in action modes and is an anti-breast cancer compound acting on an estrogen receptor and histone histone deacetylase dual target sites.

A oxo bridge Shuanghuan -[ 2.2.1]- heptylene class compound and use thereof

The invention belongs to the technical field of medicines, and particularly discloses an oxygen-bridge bicyclo-[2.2.1]-heptylene compound comprising N-hydroxy-N'-phenyloctanediamide (SAHA) or a like structure, wherein the oxygen-bridge bicyclo-[2.2.1]-heptylene compound has an activity of resisting breast cancer. 3-(4-hydroxy penyl)-4-octanedioic acid monoanilide-furan and a vinyl sulphonate derivative are taken as raw materials and are reacted without a solvent or a catalyst at the temperature of 90 DEG C for 3 hours to further prepare the oxygen-bridge bicyclo-[2.2.1]-heptylene compound comprising the octanedioic acid monoanilide, and then the compound is reacted with oxammonium hydrochloride to obtain the oxygen-bridge bicyclo-[2.2.1]-heptylene compound comprising the N-hydroxy-N'-phenyloctanediamide. The experiments in vitro show that the oxygen-bridge bicyclo-[2.2.1]-heptylene compound has a great inhibitory activity on an MCF-7 cell in comparison to an existing anti-breast-cancer medicine tamoxifen.

Thiophene-core estrogen receptor ligands having superagonist activity

To probe the importance of the heterocyclic core of estrogen receptor (ER) ligands, we prepared a series of thiophene-core ligands by Suzuki cross-coupling of aryl boronic acids with bromo-thiophenes and we assessed their receptor binding and cell biological activities. The disposition of the phenol substituents on the thiophene core, at alternate or adjacent sites, and the nature of substituents on these phenols, all contribute to binding affinity and subtype selectivity. Most of the bis(hydroxyphenyl)-thiophenes were ERβ selective, whereas the tris(hydroxyphenyl)-thiophenes were ERα selective; analogous furan-core compounds generally have lower affinity and less selectivity. Some diarylthiophenes show distinct superagonist activity in reporter gene assays, giving maximal activities 2-3 times that of estradiol, and modeling suggests that these ligands have a different interaction with a hydrogen-bonding residue in helix-11. Ligand-core modification may be a new strategy for developing ER ligands whose selectivity is based on having transcriptional activity greater than that of estradiol.

Development of Selective Estrogen Receptor Modulator (SERM)-Like Activity Through an Indirect Mechanism of Estrogen Receptor Antagonism: Defining the Binding Mode of 7-Oxabicyclo[2.2.1]hept-5-ene Scaffold Core Ligands

Previously, we discovered estrogen receptor (ER) ligands with a novel three-dimensional oxabicyclo[2.2.1]heptene core scaffold and good ER binding affinity act as partial agonists via small alkyl ester substitutions on the bicyclic core that indirectly mo

Synthesis and evaluation of estrogen receptor ligands with bridged oxabicyclic cores containing a diarylethylene motif: Estrogen antagonists of unusual structure

A new series of ligands for the estrogen receptor (ER) based on a three-dimensional structural motif consisting of a bridged oxabicyclic core (7-oxabicyclo[2.2.1]heptene or heptadiene) were synthesized and examined for their receptor binding activity and as regulators of transcription through the two ER subtypes, ERα and ERβ. The prototypical ligands also contain a 1,2-diarylethylene motif, common to many nonsteroidal estrogens, as an embellishment on the oxabicyclic core. Thus, these ligands bear peripheral groups typically found in ER ligands, built here upon an overall three-dimensional core topology that is unusual for these targets. Most of these compounds were conveniently synthesized by a Diels-Alder reaction of various 3,4-diarylfurans with a variety of dienophiles, neat and under mild conditions in the absence of catalysts. Some of the synthesized compounds display good binding affinity for the ER, and in transcription assays, the highest affinity compounds are antagonists on both ERs. Molecular modeling studies suggest a structural basis for the antagonist activity of these compounds. These compounds, based on the bicyclo[2.2.1]core system, expand the structural diversity of ligands that can be antagonists for the estrogen receptors.