A pharmaceutical composition for treating cancer, especially liver cancer

A technology for the treatment of liver cancer and drugs, applied in drug combinations, pharmaceutical formulations, anti-tumor drugs, etc., can solve the problems of no other diseases, such as expanded application reports of cancer, and achieve good application prospects and value, and the effect of good anti-liver cancer activity.

Active Publication Date: 2019-05-24
THE SECOND HOSPITAL AFFILIATED TO WENZHOU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] As mentioned above, some purposes of indazoloquinazolinone compounds are disclosed in the prior art, but most of these uses are only limited to its fluorescent properties and the field of respiratory system disease treatment at present, but not for other diseases, especially cancer ( more particularly liver cancer) reported any extended application

Method used

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  • A pharmaceutical composition for treating cancer, especially liver cancer
  • A pharmaceutical composition for treating cancer, especially liver cancer
  • A pharmaceutical composition for treating cancer, especially liver cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Cytotoxicity GI on different cell lines 50

[0035] Experimental procedure: Miapaca-2 used herein is pancreatic cancer cells, Hela is human cervical cancer cells and Hep3B is human liver cancer cells. Each cell was grown in DMEM culture medium containing 10% fetal bovine serum by mass percentage, the antibiotic concentration in the culture medium was 100 μ / ml penicillin and 100 μg / ml streptomycin, and the cell culture was carried out at a temperature of 37° C. carried out in an incubator with a volume concentration of 5%.

[0036] Cells were evenly plated on a 96-well plate at a density of approximately 5×10 3 , add 200 μl complete medium to each well, and culture overnight. After the cells adhere to the wall and grow smoothly, add serum-free DMEM medium containing 25 μM drug and treat for 24 hours. The PBS (phosphate buffer) solution of MTT was prepared so that the concentration of MTT was 5 μg / m, added to serum-free medium and incubated at 37° C. for 4 ...

Embodiment 2

[0041] Example 2: Effects on HL-7702 and Hep3B cell apoptosis and related protein expression

[0042] Experimental procedure: the HL-7702 used here are human normal hepatocytes, and the culture conditions are consistent with the culture of Hep3B mentioned above.

[0043] Hep3B and HL-7702 cells were treated with compounds for 24 hours, trypsinized and harvested. Rinse three times with pre-cooled PBS, add 100 μl cell lysate RIPA and lyse on ice for 30 minutes, vortex from time to time. After centrifugation at 4°C, the supernatant was collected and the protein concentration was determined by the Bradford method. After calculating the appropriate loading concentration, add the protein sample to an appropriate ratio of loading buffer and denature at high temperature for 5 minutes. A polyacrylamide gel with a mass content of 10% of the separating gel and 5% of the stacking gel was configured, and the sample was loaded and run with a current of 40mA and a time of 2 hours. The pro...

Embodiment 3

[0047] Example 3: Effects on Mitochondrial Membrane Potential and Voltage-Dependent Anion Channel 1 (VDAC1) Protein in HL-7702 and Hep3B Cells

[0048] Experimental procedure: the mitochondrial membrane potential (MMP) of the cells was measured using the JC-1 cell apoptosis detection kit. JC=1, as a specific fluorescent probe for mitochondrial membrane potential, has two forms. It is a monomer at a low potential and emits green fluorescence; it aggregates into a complex at a high potential and emits red fluorescence. The complete mitochondrial membrane potential is at a high potential, and once the electron chain is damaged, that is, cell apoptosis occurs, the mitochondrial membrane potential will decrease. Fluorescence changes of JC-1 can be considered as an indicator of mitochondrial membrane status.

[0049] After HL-7702 cells and Hep3B cells were treated with drugs for 24 hours, the cells were trypsinized and collected. Rinse twice with PBS, incubate with JC-1 dye worki...

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PUM

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Abstract

The invention relates to a pharmaceutical composition for treating cancer, especially liver cancer. The composition comprises a quinazolinoindazole derivative shown as the formula (I) in the description. In the formula, R1 and R3 are independently selected from H, halogen, or C1-C6 alkyl, and R2 is selected from H, halogen, C1-C6 alkyl, or halogenated C1-C6 alkyl. The quinazolinoindazole derivative is excellent in pharmaceutical activity of treating cancer, especially excellent in liver cancer treatment effect. The composition doesn't affect the normal physiological function of normal hepatocyte, and has bright application prospects and great potential in the field of liver cancer treatment.

Description

technical field [0001] The invention provides a pharmaceutical composition, more specifically, provides a pharmaceutical composition for treating cancer, especially liver cancer, and belongs to the field of medicinal chemistry. Background technique [0002] As a very important class of nitrogen-containing heterocyclic compounds, quinazolinone derivatives are widely used in medicine, agriculture, chemical industry and other industries. At present, many quinazolinone drugs have been widely used in real life, such as antihypertensive drug prazosin, diuretic drug toluene quinazolone and so on. [0003] As one of the quinazolinone derivatives, quinazolinone indazole derivatives are also an important class of nitrogen-containing condensed ring compounds, which have a variety of specific properties, such as: [0004] Disclosed in Weiguang Yang et al. (Palladium-Catalyzed Cascade Reaction of 2-Amino-N'-arylbenzohydrazides with Triethyl Orthobenzoates To Construct Indazolo[3,2-b]qui...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/519A61P35/00
CPCA61K31/519A61K2300/00
Inventor 王志翊邓应彬王志斌翁杰吴和陈婵乔瑞陈大庆
Owner THE SECOND HOSPITAL AFFILIATED TO WENZHOU MEDICAL COLLEGE
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