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New anti-tumor use of iso-oxazoline derivates

An isoxazolyl and compound technology, which is applied in the field of anti-tumor drugs, and can solve problems such as new uses of anti-tumor drugs that are not involved

Inactive Publication Date: 2011-07-27
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The isoxazoline derivatives described in Chinese patent CN101070308 disclose compounds of the general formula I structure, their preparation methods, pharmaceutical compositions containing them, and their use in the preparation of antibacterial drugs. New uses of cancer drugs

Method used

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  • New anti-tumor use of iso-oxazoline derivates
  • New anti-tumor use of iso-oxazoline derivates
  • New anti-tumor use of iso-oxazoline derivates

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0086] Embodiment 1 (reference embodiment)

[0087] Preparation of Isoxazoline Derivatives

[0088] The compound of general formula I of the present invention is synthesized through the following steps:

[0089]

[0090] Wherein, X and Y are simultaneously or respectively chlorine and bromine, and R 1 , R 2 , R 3 , R 4 , R 5 The definition is the same as above. The compound of general formula I and the pharmaceutically acceptable salt thereof in the present invention are prepared by referring to the methods provided by WO99 / 41244 and CN101070308.

Embodiment 2

[0092] Antitumor Effects of Isoxazoline Derivatives in Vitro

[0093] (1) Experimental method:

[0094] The classic cytotoxic activity in vitro detection method MTT method was used to detect the cell proliferation toxicity of isoxazoline derivatives to human tumor cells cultured in vitro.

[0095] (2) Experimental materials:

[0096] Experimental samples: Isoxazoline derivatives were provided by the Drug Innovation Research Center of Tianjin Pharmaceutical Research Institute. During the experiment, the sample was dissolved with DMSO, and the serum-free DMEM medium was diluted to the required concentration, and part of the sample solution was suspended.

[0097] Main reagents: MTT, subpackaged by Amresco, batch number: 04M0904. Complete DMEM medium, product of Gibco Company, lot number: 1290007. Calf serum, Lanzhou Minhai Biology, batch number: 20060509. Trypsin, subpackaged by Amresco Company, batch number: 016B0604; fluorouracil injection, 0.25g / 10ml (branch), batch numb...

Embodiment 3

[0110] (1) Experimental materials:

[0111] Sample: I-17, provided by the Drug Innovation Research Center of Tianjin Institute of Pharmaceutical Research.

[0112] Cell lines: sarcoma S180 cells and liver cancer H22 cells were purchased from Shanghai Cell Institute, Chinese Academy of Sciences.

[0113] Positive control drug: cyclophosphamide, batch number: 07020121, Jiangsu Hengrui Medicine Co., Ltd.

[0114] Instrument: PB303-N thousandth electronic balance, produced by Mettler-Toledo.

[0115] Animals: Kunming mice, SPF grade, half male and half female, weighing 18-22 g, purchased from the Institute of Radiological Medicine, Chinese Academy of Medical Sciences, certificate number: SCXK (Jin) 2005-0001.

[0116] (2) Experimental method:

[0117] Take tumor-bearing mice that were inoculated with tumor strains in the peritoneal cavity for 9 days. The tumors grow well and the abdomen is obviously distended. Aseptically absorb ascites, dilute it with 1:3 normal saline to make...

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Abstract

The invention relates to the medicine field related to resistance to tumor and provides isoxazole oxazoline derivative with the structure of the general formula (1) and the pharmaceutically acceptable salt and the new application of the drug combination in preparing anti-tumor drugs, wherein, all the groups are defined as the specification.

Description

technical field [0001] The invention belongs to the field of anti-tumor related medicines, and more specifically relates to the new application of isoxazoline derivatives as anti-tumor medicines and the pharmaceutical composition containing them. Background technique [0002] Cancer is one of the most important killers of human health, and its death rate ranks first in my country and second in the world. According to the statistics of the World Health Organization, the number of cancer deaths in the world in 2007 reached 7.9 million (accounting for about 13% of all deaths), and lung cancer, gastric cancer, liver cancer, colon cancer and breast cancer are the main culprits of most cancer deaths every year. In recent years, the incidence of cancer has been increasing year by year due to the increasing risk of cancer risk factors such as urban air pollution, overweight or obesity, alcohol and tobacco abuse. In developing countries, as deaths from infectious diseases and child ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/496A61P35/00
Inventor 刘默刘巍刘冰妮刘登科刘颖徐为人成碟张存彦汤立达
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH