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Application of compound in treatment of lung cancer

A compound and lung cancer technology, applied in the direction of active ingredients of heterocyclic compounds, medical preparations containing active ingredients, drug combinations, etc., can solve problems that affect health, increase the prevalence of lung cancer, and adverse health effects on the surrounding population

Active Publication Date: 2018-02-06
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, smoking not only directly affects the health of the individual, but also has a negative impact on the health of the surrounding population, resulting in a significant increase in the incidence of lung cancer among passive smokers.

Method used

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  • Application of compound in treatment of lung cancer
  • Application of compound in treatment of lung cancer
  • Application of compound in treatment of lung cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1. Preparation of compound 1-92

[0038]

[0039] Take Intermediate A1 in a 100ml round bottom flask, add 198mg Pd(dppf) 2 .DCM, 2g potassium phosphate and 1.2g p-trifluoromethylthiophenylboronic acid pinacol ester, add 10ml toluene, under argon protection, react at 100℃ for 12h, spin dry the solvent, add 100ml water, and extract with 20ml dichloromethane Twice, pass through a silica gel column with petroleum ether: ethyl acetate = 30:1 to obtain 1 g of intermediate A3 (colorless liquid) with a yield of 64%.

[0040] Take 1g of Intermediate A3 and 650mg of Intermediate A4 in a 25ml round-bottomed flask, add 240mg of p-toluenesulfonic acid monohydrate and 10ml of n-butanol, react at 130℃ for 16h, spin dry the solvent under reduced pressure, add water, and use 20ml ethyl acetate Extracted twice, passed through a silica gel column with ethyl acetate: petroleum ether=1:1 to obtain 320 mg of compound 1 (white solid), with a total yield of 24%.

[0041] The characterization...

Embodiment 2

[0044] Example 2. Study on the inhibitory effect of compounds on lung cancer

[0045] Reagents and materials used: R1640 medium (Thermo), DMEM medium (Thermo), FBS (Thermo), DMEM / F12 medium (Thermo), B27 (Thermo), EGF (Peprotech), bFGF (Peprotech), PBS ( Thermo), 0.25% pancreatin (Thermo), DMSO (Sigma), MTS (Promega), PMS (Sigma). 96-well low-adsorption cell culture plate (Corning), 96-well conventional V-shaped cell culture plate (NEST), 96-well conventional flat-bottom cell culture plate (NEST), 6cm, 10cm conventional cell culture dishes (NEST), 15\50ml centrifuge tube (NEST), 5\10ml pipette (NEST).

[0046] Instruments used: high-content live cell screening analyzer (CellomicArrayScan VTI 700, ThermoScientific Cellomics); multifunctional microplate reader (EnVision, PerkinElmer); optical microscope (ECLIPSETi Microscope, Nikon); centrifuge (Heraeus Multifugeⅹ1R, Thermo Scientific Cellomics); Liquid device (Brand, Germany).

[0047] 1. Inhibitory activity of compound 1-92 (1 μM)...

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Abstract

The invention discloses an application of a compound in treatment of lung cancer. The compound has the structural formula shown in formula I or formula II. The compound shown in formula I, the compound shown in formula II and pharmacologically acceptable salt or prodrugs of the compounds can be used for preventing and / or treating the lung cancer. The lung cancer specifically can be small cell lungcancer or non-small cell lung cancer. Tests prove that the compound shown in formula I, the compound shown in formula II and pharmacologically acceptable salt or prodrugs of the compounds all have aninhibition function on small cell lung cancer or non-small cell lung cancer of the lung cancer and have the inhibition activity superior to that of existing inhibitors.

Description

Technical field [0001] The present invention relates to the application of a compound in the treatment of lung cancer. Background technique [0002] Lung cancer is one of the malignant tumors with the fastest increase in morbidity and mortality and the greatest threat to the health and life of the population. In the past 50 years, many countries have reported that the incidence and mortality of lung cancer have increased significantly. The incidence and mortality of lung cancer in men are the first of all malignant tumors, the incidence of women is the second, and the mortality is the second. The cause of lung cancer is still not completely clear. A large amount of data shows that long-term heavy smoking is very closely related to the occurrence of lung cancer. Existing studies have shown that the probability of long-term large numbers of smokers suffering from lung cancer is 10 to 20 times that of non-smokers. The younger the smoker, the higher the probability of lung cancer. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/47A61K31/352A61K31/4709A61P35/00
CPCA61K31/352A61K31/47A61K31/4709
Inventor 饶燏郭伟杨毅庆高红英
Owner TSINGHUA UNIV