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Preparation method of benzoyl-containing acrylic acid podophyllotoxin ester derivative and application of benzoyl-containing acrylic acid podophyllotoxin ester derivative in tumor suppression

A technology of benzoylacrylic acid and podophyllotoxin, which is applied in the direction of antineoplastic drugs, organic chemical methods, drug combinations, etc., can solve the problems of strong toxicity, application limitations, and lack of tumor tissue selectivity, and achieve low toxicity and strong side effects. Inhibitory activity, effect of significant tumor cell inhibitory activity

Active Publication Date: 2021-07-30
济宁市第一人民医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, its application is limited due to its strong toxicity to normal cells, severe gastrointestinal reactions, and lack of selectivity for tumor tissues.

Method used

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  • Preparation method of benzoyl-containing acrylic acid podophyllotoxin ester derivative and application of benzoyl-containing acrylic acid podophyllotoxin ester derivative in tumor suppression
  • Preparation method of benzoyl-containing acrylic acid podophyllotoxin ester derivative and application of benzoyl-containing acrylic acid podophyllotoxin ester derivative in tumor suppression
  • Preparation method of benzoyl-containing acrylic acid podophyllotoxin ester derivative and application of benzoyl-containing acrylic acid podophyllotoxin ester derivative in tumor suppression

Examples

Experimental program
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Effect test

example 1

[0025] Example 1: Preparation of acetate derivatives of formula I benzoyl acrylic acid

[0026] The catalyst 0.02 mol of anhydrous aluminum chloride and 0.01 mol of syartnutic anhydride was dissolved in 40 mL of flask, stirred at room temperature for 10 min, allowing anhydrous aluminum chloride and tobi-oxyleneic anhydride to fully dissolve, and then 0.01 mol The xylene was slowly added dropwise to the solution system, and the color of the solution gradually became a yellowish brown. The above reaction system was stirred under room temperature for 12 h, and the TCL codes were detected to detect the reaction progress. After the reaction was completed, the concentration of 20% dilute hydrochloric acid was added dropwise to the reaction system to the solution pH = 6 to 7 (neutralized acidity), followed by extraction separation using 100 ml of liquid solution (addition of saturated saline to prevent emulsification) . Extraction three times. The lower dichloromethane solvent layer was ...

example 2

[0042] Example 2: Application of Toxin Toxide Derivatives Toxide Derivatives

[0043] Taking MCF-7, H460, HGC-27, A549 and 293T human normal renal epithelial cell lines as the detection strain, MTT colorimetric method is a detection method, by tumors of ghostane-derived derivatives in formula I benzoyl acrylic acid Cell inhibitory activity studies have found that the novel structure derivatives have significant inhibitory activity in vitro tumor cells. See the results figure 1 , 2 3, 4.

example 3

[0044] Example 3: Compound 12C significantly induces HGC-27 apoptosis

[0045] The compound 12c was used to HGC-27 cells at different concentrations (0, 0.2, 0.6, 1.2 μm), treated 24 h, collected cells, centrifugation, washed twice with PBS; bindingBuffer in PI / FITC dye kits. The cells were added to 5 μl of FITC and 10 μl Pi, respectively, and the anti-lighting was stained with 4 minutes, and the cell apoptosis was detected with flow cytometry. See the results Image 6 . The novel derivatives of this type of structure can significantly promote the apoptosis of HGC-27 in human gastric cancer cells.

[0046] The benzoyl acrylic acid-ghostophenin ester derived in the present invention can be prepared into an anti-tumor drug.

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Abstract

The invention discloses a benzenesulfonamide phenylacetic acid podophyllotoxin carboxylic ester derivative as well as a synthesis method and application thereof, belongs to the technical field of chemical pharmacy, and particularly relates to a podophyllotoxin derivative and application thereof in tumor inhibition. Corresponding benzenesulfonamide phenylacetic acid is connected with podophyllotoxin through a synthesis means to obtain corresponding ester derivatives, and in-vitro anti-tumor activity research shows that the podophyllotoxin carboxylic ester derivatives have very strong inhibitory activity on tumor cell strains.

Description

[0001] First, technical field [0002] The present invention belongs to the field of chemical pharmaceutical technology, and more particularly to the preparation of a benzoyl acrylic acid stexin ester derivative and its application in tumor suppression. [0003] Second, background technology [0004] Podophyllotoxin, PPTs belong to cyclooxylates in ambitulin compound, with anti-tumor, antiviral, anti-inflammatory, anti-parasitic, and other biological activity, wherein the anti-tumor activity is most significant and subject to domestic The extensive attention of foreign lasters. At present, its derivatives deactivated or replacement has been successfully used for clinical treatment of various tumor diseases such as small cell lung cancer, lymphoma and gastric adenocarcinoma. However, due to its strong gastrointestinal reactions and lack of selectivity to tumor tissue, it has been restricted due to severe gastrointestinal reactions. This causes the study of C-4 position structural mod...

Claims

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Application Information

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IPC IPC(8): C07D493/04A61P35/00
CPCC07D493/04A61P35/00C07B2200/07
Inventor 江沛孙文学赵世媛王长水刘蒙蒙
Owner 济宁市第一人民医院
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