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Selective modulator of human estrogen receptor alpha36 subtype

An estrogen receptor, selective technology, applied in the direction of organic active ingredients, pharmaceutical formulations, anti-tumor drugs, etc., to achieve the effect of broad application prospects and broad transformation space

Inactive Publication Date: 2014-05-07
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

There are no reports on the application of estrogen receptors

Method used

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  • Selective modulator of human estrogen receptor alpha36 subtype
  • Selective modulator of human estrogen receptor alpha36 subtype
  • Selective modulator of human estrogen receptor alpha36 subtype

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Experimental program
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Embodiment

[0026] 1. Experimental materials

[0027] According to the structure of formula I, the compound with the structure shown in Table 1 was purchased, and the sample was purchased from Enamine Reagent Co., Ltd., and dissolved in DMSO as a solvent. IC162 is a molecule known to specifically act on the α36 subtype of estrogen receptor and can lead to inhibition of cell activity, provided by Beijing Shenaoji Pharmaceutical Technology Co., Ltd.

[0028] Table 1 Table of compounds used in experiments

[0029]

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Abstract

The present invention discloses a selective modulator of a human estrogen receptor alpha36 subtype, and a use of the selective modulator in preparation of drugs for prevention and treatment of diseases caused by estrogen receptor abnormality. According to the present invention, the selected compounds can be selectively bound with the estrogen receptor alpha36 subtype in theory; experiment results confirm that: the compounds can activate the ERK channel, inhibit the cancer cell cycle, and initiate apoptosis through the estrogen receptor alpha36 subtype so as to provide inhibition effects for cancer cells, wherein the cell growth inhibition activity of the compounds is superior to the cell growth inhibition activity of a variety of the currently-researched selective modulators of the estrogen receptor alpha36 subtype; and with the skeleton diversity of the compounds, the target compound has advantages of broad transformation space, synthetic route choice and the like, and the application prospects are broad.

Description

technical field [0001] The present invention relates to an estrogen receptor regulator, in particular to a human estrogen receptor α36 subtype selective regulator, and the use of the regulator in the preparation and prevention of diseases caused by estrogen receptor abnormalities use. Background technique [0002] Estrogen is an essential substance that regulates human development and normal physiological functions. Studies have found that the regulatory mechanism centered on estrogen receptors is closely related to body development and the regulation of many systems in the body, especially bone metabolism, cardiovascular system, and cell cycle regulation. [0003] Estrogen acts mainly through three subtypes of estrogen receptors, namely α subtype, β subtype, and the recently reported α36 subtype. Drugs targeting estrogen receptor α subtype, such as estradiol and tamoxifen, have been widely and long-term used in the prevention and treatment of estrogen replacement therapy ...

Claims

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Application Information

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IPC IPC(8): A61K31/472A61K31/433A61P5/24A61P35/00A61P19/10A61P9/00
Inventor 刘振明王东金宏威韩蕴张亮仁
Owner PEKING UNIV
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