Gamma-hydroxy olic acid ester derivatives and use thereof in preparation of antitumor medicines

A kind of hydroxyalkynoate, antitumor drug technology, applied in the field of biochemistry

Active Publication Date: 2012-01-04
LANZHOU UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the asymmetric synthesis of chiral propargyl alcohols has developed rapidly in the past ten years, the development of such asymmetric synthesis methods is limited to the construction of simple structures of A, B, and C, and γ-hydroxypropiolic acid (F ) asymmetric synthesis has been greatly limited due to its lively structure

Method used

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  • Gamma-hydroxy olic acid ester derivatives and use thereof in preparation of antitumor medicines
  • Gamma-hydroxy olic acid ester derivatives and use thereof in preparation of antitumor medicines
  • Gamma-hydroxy olic acid ester derivatives and use thereof in preparation of antitumor medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0052] The structure, synthesis and antitumor activity of the γ-hydroxyalkynoate derivatives of the present invention will be described in detail below through specific examples.

[0053] In Examples 1 to 43, the structure of the gamma-hydroxy alkynoate derivative is as follows:

[0054]

[0055] Its synthetic method can select the synthetic method of aforementioned chiral (R)-γ-hydroxy alkynoate and the synthetic method of chiral (S)-γ-hydroxy alkynoate according to different configurations, and according to different compounds, in Pay attention to the selection of corresponding aldehydes during the synthesis process. In Examples 1-43, the configuration, characterization and other characteristics of the γ-hydroxyalkynoate derivatives are shown in Table 1.

[0056] Table 1.

[0057]

[0058]

[0059]

[0060]

[0061]

[0062]

[0063]

[0064]

[0065]

[0066] In Examples 44 to 60, the structures of gamma-hydroxy alkynoate derivatives are as f...

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Abstract

The invention discloses gamma-hydroxy olic acid ester derivatives having antitumor activity and the use thereof in the preparation of antitumor medicines, and belongs to the field of biochemical technology. The structure of the gamma-hydroxy olic acid ester derivatives is shown in the description. The results of classic methyl thiazolyl tetrazolium (MTT) tumor cell medicine screening experiments, AnnexinV/PI double-staining cell apoptosis measurement experiments, cell periodical detection experiments and in-vivo antitumor experiments prove that the gamma-hydroxy olic acid ester derivatives have proliferation inhibition effects on breast cancer, bladder cancer and liver cancer and can be used in the preparation of antitumor medicines as an active ingredient.

Description

technical field [0001] The invention belongs to the technical field of biochemistry and relates to a gamma-hydroxy alkynoate derivative; the invention also relates to the application of the gamma-hydroxy alkynoate derivative in the preparation of antitumor drugs. Background technique [0002] Cancer has become the main killer threatening human life and health. According to reports, the global cancer incidence is on the rise, and will increase by 50% in the next ten years. The incidence of cancer in my country has increased by nearly 70% over the past two decades, while the mortality rate has increased by nearly 30%. With the rapid development of organic chemistry, chemotherapy has become one of the fastest growing fields in tumor treatment. It is not only an auxiliary means of tumor treatment, but also has gradually developed into one of the most common and effective methods and means. Therefore, the isolation, design, synthesis and transformation of compounds with potent...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/732C07C69/734C07C205/56C07C235/34C07C255/57C07D333/24C07D307/54A61K31/22A61K31/165A61K31/277A61K31/381A61K31/341A61P35/00A61P35/02
Inventor 王锐林利宋虹瑾
Owner LANZHOU UNIVERSITY
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