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A kind of tumor angiogenesis inhibitor hexanolone and its preparation method and application

A technology of tumor blood vessels and inhibitors, applied in the field of medicine, can solve problems such as new quinolinones that have not been seen

Active Publication Date: 2016-03-30
CHONGQING UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] So far, there is no novel quinolinone used for the treatment of tumors described in the present invention

Method used

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  • A kind of tumor angiogenesis inhibitor hexanolone and its preparation method and application
  • A kind of tumor angiogenesis inhibitor hexanolone and its preparation method and application
  • A kind of tumor angiogenesis inhibitor hexanolone and its preparation method and application

Examples

Experimental program
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Embodiment 1

[0029] Example 1, preparing and synthesizing the tumor angiogenesis inhibitor hexanolinone, comprising the following steps:

[0030] 1. Take 13mmol of o-aminopropiophenone and 20mmol of heptanoyl chloride, put them in a 250ml double-neck round bottom flask, add 18mmol of pyridine, 60-80ml of dichloromethane, stir and react at room temperature for 4-20 hours, add saturated ammonium chloride solution for 60 -100ml, take the organic phase, concentrate under reduced pressure, conduct silica gel column chromatography on the residue, collect the target object, concentrate under reduced pressure, and dry to obtain heptanylaminopropiophenone;

[0031] 2. Put 11 mmol of heptanylaminopropiophenone obtained in step 1 into a 250 ml double-neck round bottom flask, add 30-40 mmol of sodium tert-butyl alkoxide, 180-240 ml of anhydrous organic solvent, reflux for 4-36 hours, and decompress Concentrate to recover ethanol, add 100-200ml of water to elute once, and the residue is subjected to si...

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PUM

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Abstract

The present invention provides a tumor angiogenesis inhibitor jilintong, a preparation method and uses thereof, and belongs to the technical field of medicine. Specifically the name is 2-hexa alkyl-3-methyl-4(1H)-quinolinone, the chemical formula is C16H21NO, and the tumor angiogenesis inhibitor is named jilintong. The invention further provides a preparation method of the compound, and a tumor angiogenesis inhibition effect of the compound. The jilintong is total synthesis. The compound represented by a formula I provides an inhibition effect for tumor angiogenesis, and has safety so as to provide possibility for development of a new tumor treatment drug.

Description

technical field [0001] The invention provides a novel quinolinone compound with tumor angiogenesis inhibitory effect, its preparation method and application, belonging to the technical field of medicine. Background technique [0002] Angiogenesis is the process by which tissues utilize existing blood vessels to generate new blood vessels. The primary tumor has the ability to induce angiogenesis, and its growth and metastasis depend on the formation of tumor angiogenesis. Tumor angiogenesis has become a new and promising target for anti-tumor therapy. Drugs that destroy or inhibit tumor angiogenesis and effectively prevent tumor growth and metastasis are called tumor angiogenesis inhibitors (tumorangiogenesisinhibtor, TAI). [0003] Compared with traditional cytotoxic drugs, TAI has its advantages or characteristics, such as better specificity; it can play a direct role, and the effect can be amplified; it is not easy to produce drug resistance; less toxic and side effects,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D215/233A61P35/00
Inventor 胥秀英李敖郑一敏王锐刘红张心蕊陈海芹
Owner CHONGQING UNIV OF TECH
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