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Compound based on inhibiting histone demethylase as well as preparation method thereof and application in resisting gastric carcinoma

A methylase compound and compound technology, applied in the field of biomedicine, can solve the problems of poor cell permeability, complicated interpretation of biological research, lack of selectivity, etc., and achieve reduced migration ability, novel structure, and inhibition of enzyme activity. Effect

Inactive Publication Date: 2019-03-12
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Other molecules inhibit KDMs in a competitive manner with 2-OG, such as N-oxalylglycine (NOG), 2,4-pyridinedicarboxylic acid (2,4-PDA), lack of selectivity or poor cell permeability, making the use of these Complicating the Interpretation of Biological Studies of Compounds

Method used

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  • Compound based on inhibiting histone demethylase as well as preparation method thereof and application in resisting gastric carcinoma
  • Compound based on inhibiting histone demethylase as well as preparation method thereof and application in resisting gastric carcinoma
  • Compound based on inhibiting histone demethylase as well as preparation method thereof and application in resisting gastric carcinoma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] The preparation of embodiment 1 WXSA-082B

[0031] One, the preparation of intermediate 2

[0032] Weigh (2,2'-bipyridyl)-4,4'-dicarboxylic acid dimethyl ester (0.55 g, 2.0 mmol) into a conical flask, add tetrahydrofuran:methanol=1:1 total 40mL, stir at room temperature for 15 Minutes; then 2 mL of 1 mol / L potassium hydroxide aqueous solution was added dropwise into the Erlenmeyer flask under an ice bath, and continued stirring at room temperature overnight. After the reaction was completed, the solvent was evaporated to dryness under reduced pressure, 50 mL of water was added thereto, and then 1 mol / L of dilute hydrochloric acid was added until the solid was precipitated, the filter residue was taken by suction filtration, 40 mL of dichloromethane was added to the filter residue, and the filter residue was taken by suction filtration to obtain the crude product of Intermediate 2 . White solid, yield 18%.

[0033] .

[0034] 2. Preparation of WXSA-082B

[0035] W...

Embodiment 2

[0038] Example 2 Detecting the Effect of Compounds on RBP2 Enzyme Substrates in Gastric Cancer Cells (Western blot)

[0039] Purpose:

[0040] The effect of the test compound on the RBP2 enzyme substrate H3K4me3

[0041] Experimental Materials:

[0042] RPMI 1640 medium was purchased from Gibco;

[0043] Fetal bovine serum was purchased from Gibco;

[0044] DMSO was purchased from Sigma;

[0045] EpiQuik Total Histone Extraction Kit (OP-0006-100) was purchased from Epigentek Group;

[0046] Pierce ® BCA Protein Assay Kit was purchased from Thermo fisher scientific company

[0047] laboratory apparatus:

[0048] HF safe biological safety cabinet,

[0049] MCO-15AC carbon dioxide incubator, Japan Sanyo SANYO,

[0050] Polyacrylamide gel vertical electrophoresis tank, Liuyi Instrument Factory, Beijing, China

[0051] Test drug:

[0052] Compound WXSA-082B was prepared as a stock solution with DMSO, with a final concentration of 200mM. When used, it was diluted with in...

Embodiment 3

[0062] Example 3 Detection of compound's effect on migration ability in gastric cancer cells (Transwell)

[0063] Purpose:

[0064] The effect of detection compounds on the migration ability of gastric cancer cells

[0065] Experimental Materials:

[0066] RPMI 1640 medium was purchased from Gibco;

[0067] Fetal bovine serum was purchased from Gibco;

[0068] DMSO was purchased from Sigma;

[0069] Corning Transwell 3542 chamber was purchased from Beijing Suo Laibao Technology Co., Ltd.

[0070] laboratory apparatus:

[0071] HF safe biological safety cabinet,

[0072] MCO-15AC carbon dioxide incubator, Japan Sanyo SANYO,

[0073] Olympus CKX53 biological microscope, Shanghai Puhe Optoelectronics Technology Co., Ltd.,

[0074] Test drug:

[0075] For compound WXSA-082B, the sample was prepared into a mother solution with DMSO, with a final concentration of 200mM. When used, it was diluted with incomplete medium, and the final concentration of DMSO was not more than 0...

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Abstract

The invention provides a compound WXSA-082B based on inhibiting histone demethylase, further provides a preparation method thereof. Tests shown that the compound can enable H3K4me3 protein level in human gastric carcinoma cell BGC-823 to increase obviously, has obvious RBP2 enzyme activity inhibiting effect, and can reduce the transfer ability of the human gastric carcinoma cell BGC-823. The compound provided by the invention can be applied to preparation of anti-gastric carcinoma drugs serving as a gastric carcinoma inhibitor. The structure of the compound is as follows: (the structure is shown in the description).

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and specifically relates to a compound WXSA-082B based on inhibiting histone demethylase, a preparation method thereof and an anti-gastric cancer application. Background technique [0002] Antineoplastic drugs commonly used in clinical practice are mainly cytotoxic drugs, most of which have unavoidable disadvantages such as poor selectivity, strong toxic and side effects, and easy drug resistance. In recent years, with the rapid development of life science research, various basic processes such as signal transduction in malignant tumor cells, regulation of cell cycle, induction of apoptosis, angiogenesis, and interaction between cells and extracellular matrix are being investigated. The gradual clarification has brought about a huge change in the research and development concept of anticancer drugs. Therefore, using some key enzymes / proteins related to tumor cell modification as drug targets...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/81A61K31/444A61P35/00
CPCA61P35/00C07D213/81
Inventor 贾继辉展鹏刘新泳陈春燕贾夏夏张硕俞霁王学顺
Owner SHANDONG UNIV
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