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Oxy-bridged bicyclo-heptene sulfonate compound containing five-membered nitrogen heterocycle and application thereof in preparation of anti-breast cancer drugs

A five-membered azacyclic and heptene sulfonate technology, which is applied in the field of medicine, can solve problems such as side effects and drug-resistant breast cancer, and achieve strong inhibitory activity and good inhibitory effect

Active Publication Date: 2022-05-31
WUHAN UNIV
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  • Abstract
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Problems solved by technology

Long-term use of anti-estrogen drugs such as tamoxifen can cause strong side effects and lead to drug-resistant breast cancer, study shows

Method used

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  • Oxy-bridged bicyclo-heptene sulfonate compound containing five-membered nitrogen heterocycle and application thereof in preparation of anti-breast cancer drugs
  • Oxy-bridged bicyclo-heptene sulfonate compound containing five-membered nitrogen heterocycle and application thereof in preparation of anti-breast cancer drugs
  • Oxy-bridged bicyclo-heptene sulfonate compound containing five-membered nitrogen heterocycle and application thereof in preparation of anti-breast cancer drugs

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Embodiment 1

[0100]

Embodiment 2

[0103]

Embodiment 3

[0106]

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Abstract

The invention discloses an oxygen-bridged bicyclo-heptene sulfonate compound containing five-membered nitrogen heterocycle and application of the oxygen-bridged bicyclo-heptene sulfonate compound in preparation of anti-breast cancer drugs, and belongs to the technical field of medicines. According to the invention, a furan derivative containing a five-membered nitrogen heterocyclic ring and an ethylene sulfonate derivative are used as raw materials, a catalyst is not needed, and the oxygen-bridged bicyclo-heptene compound containing the five-membered nitrogen heterocyclic ring is prepared by one step through a Diels-Alder reaction. The compound provided by the invention can well inhibit MCF-7 cells, also has good inhibitory activity on drug-resistant breast cancer cells LCC2, can well inhibit aromatase, and has an application prospect in breast cancer treatment.

Description

A kind of oxygen-bridged bicycloheptene sulfonate compound containing five-membered nitrogen heterocycle and its use Application in the preparation of anti-breast cancer drugs technical field The invention belongs to the technical field of medicine, relate to the compound based on oxygen bridge bicyclic-[2.2.1]-heptene sulfonate structure A compound, having an oxygen-bridged bicyclic-[2.2.1]-heptene sulfonate compound containing a five-membered nitrogen heterocycle and preparation thereof The method and its application in the preparation of anti-breast cancer drugs. Background technique [0002] In recent years, breast cancer has become one of the most common cancers in women. Overexpression of estrogen receptor (ER) Can lead to breast cancer, therefore, anti-estrogen drugs are constantly being developed and applied. Studies have shown that long-term use of tamoxifen Antiestrogen drugs such as xifen can cause strong side effects and lead to the development of drug-...

Claims

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Application Information

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IPC IPC(8): C07D493/08A61K31/4155A61K31/4196A61K31/4178A61P35/00A61P43/00
CPCC07D493/08A61P35/00A61P43/00
Inventor 周海兵董春娥辛丽兰李媛媛
Owner WUHAN UNIV
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