Application of ethanone compound in preparation of medicine for treating tumors

An ethyl ketone and drug technology, which is applied in the application field of ethyl ketone compounds in the preparation of tumor drugs, and achieves the effect of promoting apoptosis

Active Publication Date: 2020-09-01
JIANGNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Traditional experimental-based drug development methods, such as high-throughput screening (HTS), are difficult to find and overcome these difficulties

Method used

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  • Application of ethanone compound in preparation of medicine for treating tumors
  • Application of ethanone compound in preparation of medicine for treating tumors
  • Application of ethanone compound in preparation of medicine for treating tumors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1 (in vitro multiple tumor cell proliferation inhibition verification compound inhibits tumor cell proliferation)

[0029] The MTT assay was used to detect the inhibitory effect of the compound on the proliferation of various tumor cells.

[0030] A selective PI3Kδ / γ inhibitor IPI-145 was used as a positive control.

[0031] Blank group: use a 96-well plate and set up 3 parallel experimental groups. A variety of tumor cells (including myeloma, leukemia, lymphoma, pancreatic cancer, gastric cancer, breast cancer, ovarian cancer, and lung cancer cell lines) were spread on a 96-well plate at a density of 7,500 cells per well. After incubation for 72 hours, add 10 μL MTT was incubated for 4 hours, 100 μL MTT Buffer was added to dissolve the cell crystals, and the wavelength was detected at 560 nm absorbance.

[0032] Experimental group: 3 groups of parallel experiments were set up using a 96-well plate. 1-(5-(3-((4-chlorobenzyl)amino)-2-hydroxypropoxy)-2-methy...

Embodiment 2

[0035] Example 2 (A variety of hematological tumor cells detect the inhibitory effect of active compounds on cell proliferation)

[0036] As can be seen from Example 1, 1-(5-(3-((4-chlorobenzyl) amino)-2-hydroxypropoxy)-2-methyl-1-(p-tolyl)-1 hydrogen -Indol-3-yl)ethanone has more obvious inhibition on hematological tumors, because in such tumor cells, PI3Kγ often presents a disordered high expression state, so the following examples select myeloma cells, lymphoma cells and leukemia cells Cells and other blood tumor cells were further tested and verified, and the MTT assay was used to detect different concentrations of the compound 1-(5-(3-((4-chlorobenzyl)amino)-2-hydroxypropoxy)-2-methanol Base-1-(p-tolyl)-1hydro-indol-3-yl)ethanone inhibits the proliferation of tumor cells.

[0037] Blank group: use a 96-well plate and set up 3 parallel experimental groups. A variety of myeloma cells OPM2, LP-1, RPMI-8226, lymphoma cells U937 and leukemia cells HL-60, Jurkat, CCRF-CEM, K5...

Embodiment 3

[0041] Embodiment 3 (in vitro enzyme assay detects PI3K inhibition rate)

[0042] Detection of compound 1-(5-(3-((4-chlorobenzyl)amino)-2-hydroxypropoxy)-2-methyl-1-(p-tolyl)-1 hydrogen using ADP-Glo ​​kit Inhibitory activity of -indol-3-yl)ethanone on PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ.

[0043] The broad-spectrum PI3K inhibitor PI-103 was used as a positive control.

[0044] PI3Kγ blank group: use a 384-well plate to set up 3 parallel experimental groups. Prepare 5 μL of PI3K reaction system, each well contains 2.5 μL of PI3Kγ protein, add 2.5 μL of reaction substrate PIP2 and ATP to start the reaction, incubate at room temperature for 1 hour, use 5 μL of MgCl 2 The reagent terminated the reaction, and after incubation for 2 hours, 10 μL of ADP-Glo ​​detection reagent was added, and after incubation for 45 minutes, the fluorescence value of the reaction solution was detected by a microplate reader.

[0045] Use the same operation to prepare PI3Kα, PI3Kβ, PI3Kδ blank groups

[00...

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PUM

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Abstract

The invention discloses an application of 1-(5-(3-((4-chlorobenzyl) amino)-2-hydroxypropoxy)-2-methyl-1-(p-tolyl)-1H-indole-3-yl) ethanone or pharmaceutically acceptable salt thereof in preparation ofa medicine for treating or preventing tumor diseases. The product is used for relieving and/or adjunctively treating and/or treating myeloma, leukemia, lymphoma, pancreatic cancer, gastric cancer, breast cancer, ovarian cancer, lung cancer, liver cancer, skin cancer, rectal cancer, prostate cancer, thyroid cancer and other tumors. The 1-(5-(3-((4-chlorobenzyl) amino)-2-hydroxypropoxy)-2-methyl-1-(p-tolyl)-1 hydrogen-indole-3-yl) ethanone has a remarkable specific inhibition effect on PI3K gamma (polyisocyanurate).

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of an acetone compound in the preparation of a drug for treating tumors, which has the effect of alleviating and / or adjuvant therapy and / or treating tumor diseases. Background technique [0002] PI3K, namely phosphatidylinositol 3-kinases (phosphatidylinositol 3-kinases), is a family of kinases that also have a phosphorylated phosphatidylinositol ring. According to the selectivity of PI3K kinases for substrates, the types of regulatory subunits and the homology of amino acid sequences, PI3K family members are divided into three classes, Class I, II and III. Class I PI3K kinases have received the most intense attention compared to class II and class III PI3K kinases. According to the difference between regulatory subunits and upstream signaling pathways, class I PI3Ks can be divided into class IA (PI3Kα, PI3Kβ and PI3Kδ) and class IB (PI3Kγ). Based on the key ro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/404A61P35/00A61P35/02
CPCA61K31/404A61P35/00A61P35/02
Inventor 朱景宇金坚陈蕴蔡燕飞李侃
Owner JIANGNAN UNIV
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