Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Application of n-hydroxyphthalimide compounds in the preparation of antitumor drugs

A ‐hydroxyphthalimide and compound technology, applied in antineoplastic drugs, drug combinations, drug delivery, etc., can solve problems such as high toxicity and side effects, unreported antitumor activity, and poor pharmacokinetic properties , to achieve the effects of less toxic and side effects, inhibiting tumor growth, and convenient medication

Active Publication Date: 2018-11-13
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, some compounds still have the disadvantages of large toxic and side effects and poor pharmacokinetic properties. Therefore, it is necessary to discover new mTOR inhibitors and develop new anti-tumor drugs
[0005] So far, N-hydroxyphthalimide compounds with novel structures have not been reported as inhibitors of mTOR signaling pathway, and have anti-tumor activity

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Application of n-hydroxyphthalimide compounds in the preparation of antitumor drugs
  • Application of n-hydroxyphthalimide compounds in the preparation of antitumor drugs
  • Application of n-hydroxyphthalimide compounds in the preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] NHPI significantly inhibited mTORC1 and mTORC2 signaling pathways in different tumor cells.

[0038] 1. Cell lines: Human breast cancer BT-20 cells and human colon cancer Lovo cells were purchased from the Shanghai Cell Bank of the Chinese Academy of Sciences. Cells were placed at 37°C, 5% CO 2 Routine culture in an incubator with 10% calf serum, MEM and F12-K with a pH value of 7.4.

[0039] 2. Experimental method: take BT-20 and Lovo cells in the logarithmic growth phase, and make 3×10 5 / ml cell suspension was seeded in 6-well plate. After culturing for 24 hours, the original culture solution was aspirated after the cells adhered to the wall. Different concentrations of NHPI (purchased from Shanghai Shaoyuan Technology Co., Ltd.) were added to each well of the experimental group, and the same amount of culture solution without NHPI was added to the control group. After 24 hours, the cells were collected, the total cell protein was extracted, and subjected to SDS-P...

Embodiment 2

[0042] NHPI significantly inhibited the proliferation of different tumor cells.

[0043] 1. Cell lines: human breast cancer BT-20 cells, human colon cancer Lovo and HT-29 cells were purchased from Shanghai Cell Bank of Chinese Academy of Sciences.

[0044] 2. Experimental method: Take BT-20 cells, Lovo cells and HT-29 cells in the logarithmic growth phase, and make 1×10 4 / ml cell suspension was inoculated in a 96-well plate. After culturing for 24 hours, the original culture solution was aspirated after the cells adhered to the wall. Different concentrations of NHPI (purchased from Shanghai Shaoyuan Technology Co., Ltd.) were added to each well of the experimental group, and the same amount of culture solution without NHPI was added to each well of the control group. Set up 3 duplicate holes. After culturing each group of cells for 48 hours, 20 μl of MTS (Promega, Madison, USA) was added to each well, and after culturing for another 1-2 hours, the absorbance at 490 nm was d...

Embodiment 3

[0047] NHPI blocks Lovo cell cycle at G 2 / M period.

[0048] 1. Experimental method: Take Lovo cells in the logarithmic growth phase and make 1×10 5 / ml cell suspension was seeded in 6-well plate. After culturing for 24 hours, the original culture solution was aspirated after the cells adhered to the wall. Different concentrations of NHPI (purchased from Shanghai Shaoyuan Technology Co., Ltd.) were added to each well of the experimental group, and the same amount of culture solution without NHPI was added to the control group. At the end of the treatment, the cells were collected by trypsinization and centrifuged, washed once with pre-cooled PBS, and fixed by adding 75% ethanol (pre-cooled at -20°C) overnight. Cells were collected by centrifugation and incubated with RNase at 37°C for 30 minutes, then stained with propidium iodide (PI, Sigma), and kept in the dark at room temperature for 30 minutes, and the cell cycle was detected by flow cytometry.

[0049] 2. Experimenta...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention provides application of N-hydroxyphthalimide compounds or pharmaceutically-acceptable salt of N-hydroxyphthalimide compounds in preparation of mTOR signal path inhibitor, and application in preparation of anti-tumor medicine. It is proved that compounds N-hydroxyphthalimide (NHPI) can restrain mTOR signal paths, tumor cell proliferation can be restrained, tumor cell apoptosis can be induced, growth of breast cancer tumor transplanted subcutaneously in nude mice can be restrained, and the good in-vivo and in-vitro anti-tumor effect is displayed. The compounds are used for preparing anti-tumor medicine, a good choice is provided for the field of tumor treatment, and quite high application value is achieved.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of N-hydroxyphthalimide compounds as mTOR signaling pathway inhibitors and their application in the preparation of antitumor drugs. Background technique [0002] Tumor is a major disease that threatens human health. Most of the currently used clinical drugs are cytotoxic drugs, which have poor targeting, large toxic and side effects, and unsatisfactory therapeutic effects. Molecular targeted drugs target specific genes or gene expression products that are differentially expressed between tumor cells and normal cells, and form targeted and specific killing of tumors, which significantly improves the clinical treatment effect of tumors. [0003] Mammalian target ofrapamycin (mTOR) is a highly conserved protein belonging to the PIKK family of serine / threonine protein kinases, which can integrate signals stimulated by growth factors, amino acids, energy, etc., to r...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4035A61K31/403A61P35/00A61P35/02
CPCA61K9/0019A61K9/08A61K9/19A61K9/2059A61K9/4858A61K31/403A61K31/4035A61K47/10
Inventor 周宏宇李艳夏成峰孔令梅周安坤王敏
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com