- Oxygen bridge bicyclo - [2.2.1] - heptene compounds containing different covalent bullet structures, and preparation and application thereof
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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.
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Paragraph 0106-0108
(2021/11/03)
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- Selective estrogen receptor modulator compounds containing phenylselenyl and application of compounds in anti-breast cancer drugs
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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-(
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Paragraph 0119; 0120; 0121
(2019/05/15)
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- Oxo-bridged bicyclo-heptylene sulfonamides compound containing different alkyl chain lengths, as well as preparation method and application thereof
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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
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Paragraph 0096; 0099; 0100
(2018/12/14)
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- 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
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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.
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Paragraph 0054; 0057; 0058
(2017/09/02)
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- Oxygen bridge dicycloheptene compound containing resveratrol group and its preparation method and use method
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The invention belongs to the technical field of medicine and discloses a preparation method of an oxygen bridge dicycloheptene compound containing a resveratrol group. One of a 3-(4-hydroxyphenyl)-4-(((E)-3, 5-dihydroxystyryl)phenyl)furan compound and a 3
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Paragraph 0065; 0067; 0068
(2017/10/10)
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- A oxo bridge Shuanghuan -[ 2.2.1]- heptylene class compound and use thereof
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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.
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Paragraph 0025; 0028-0029
(2016/12/01)
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- 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
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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
- Zheng, Yangfan,Zhu, Manghong,Srinivasan, Sathish,Nwachukwu, Jerome C.,Cavett, Valerie,Min, Jian,Carlson, Kathryn E.,Wang, Pengcheng,Dong, Chune,Katzenellenbogen, John A.,Nettles, Kendall W.,Zhou, Hai-Bing
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scheme or table
p. 1094 - 1100
(2012/07/31)
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- Synthesis and evaluation of estrogen receptor ligands with bridged oxabicyclic cores containing a diarylethylene motif: Estrogen antagonists of unusual structure
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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.
- Zhou, Hai-Bing,Comninos, John S.,Stossi, Fabio,Katzenellenbogen, Benita S.,Katzenellenbogen, John A.
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p. 7261 - 7274
(2007/10/03)
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