Bibenzyl compound and its preparation method and application in the preparation of antitumor drugs

A compound and application technology, applied in the field of preparation of anti-tumor drugs, can solve the problems that there are no research reports on anti-tumor drugs of bibenzyl compounds

Inactive Publication Date: 2020-02-04
CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, there is no research report that the bibenzyl compound of the present invention is used for the preparation of antitumor drugs

Method used

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  • Bibenzyl compound and its preparation method and application in the preparation of antitumor drugs
  • Bibenzyl compound and its preparation method and application in the preparation of antitumor drugs
  • Bibenzyl compound and its preparation method and application in the preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0116] Example 1, the extraction and structural identification of compound F

[0117] (1) Extraction of medicinal materials:

[0118] Dried white and medicinal material coarse powder (3kg), reflux extraction with 95% ethanol 3 times (30L×3), 2h each time;

[0119] (2) Separation and purification of components:

[0120] 1. Ethanol extract (90L) was concentrated and dried under reduced pressure to obtain 510g of semi-solid liquid extract;

[0121] ②. Disperse the semi-solid liquid extract (500g) with water (5L), extract with ethyl acetate and n-butanol (20L) successively, combine the ethyl acetate part, recover the solvent under reduced pressure, and obtain 160g of ethyl acetate extract;

[0122] 3. Adopt silica gel column chromatography to separate ethyl acetate extract (160g), petroleum ether: acetone carries out gradient elution, and the eluent is detected by thin-layer chromatography, and obtains the elution when petroleum ether: acetone=30:1 Liquid Fr.16;

[0123] The c...

Embodiment 2

[0137] Example 2, the extraction and structural identification of compound G

[0138] (1) Extraction of medicinal materials:

[0139] Dried white and medicinal material coarse powder (3kg), reflux extraction with 95% ethanol 3 times (30L×3), 2h each time;

[0140] (2) Separation and purification of components:

[0141] 1. Ethanol extract (90L) was concentrated and dried under reduced pressure to obtain 510g of semi-solid liquid extract;

[0142] ②. Disperse the semi-solid liquid extract (500g) with water (5L), extract with ethyl acetate and n-butanol (20L) successively, combine the ethyl acetate part, recover the solvent under reduced pressure, and obtain 160g of ethyl acetate extract;

[0143] 3. Adopt silica gel column chromatography to separate ethyl acetate extract (160g), petroleum ether: acetone carries out gradient elution, and the eluent is detected by thin-layer chromatography, and obtains the elution when petroleum ether: acetone=30:1 Liquid Fr.16;

[0144] The c...

Embodiment 3

[0157] Example 3, the extraction and structural identification of compound H

[0158] (1) Extraction of medicinal materials:

[0159] Dried white and medicinal material coarse powder (3kg), reflux extraction with 95% ethanol 3 times (30L×3), 2h each time;

[0160](2) Separation and purification of components:

[0161] 1. Ethanol extract (90L) was concentrated and dried under reduced pressure to obtain 510g of semi-solid liquid extract;

[0162] ②. Disperse the semi-solid liquid extract (500g) with water (5L), extract with ethyl acetate and n-butanol (20L) successively, combine the ethyl acetate part, recover the solvent under reduced pressure, and obtain 160g of ethyl acetate extract;

[0163] 3. Adopt silica gel column chromatography to separate ethyl acetate extract (160g), petroleum ether: acetone carries out gradient elution, and the eluent is detected by thin-layer chromatography, and obtains the elution when petroleum ether: acetone=30:1 Liquid Fr.16;

[0164] The co...

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PUM

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Abstract

The invention discloses an application of a compound represented as the formula (IV), or pharmaceutically acceptable salts, crystal forms and solvates thereof, in preparation of a medicine for treating and / or preventing tumors, wherein R1, R4 and R6 are respectively and independently selected from hydrogen or a methyl group; R2, R3, R5 and R7 are respectively and independently selected from hydrogen or a structure represented as follows. The invention provides a novel application of bibenzyl compounds, and in particular, an application in preparation of a medicine for treating and / or preventing tumors. The compound has excellent inhibiting effects on tumor cells, especially, on lung carcinoma cells, wherein IC50 of the compound reaches 2-6 [mu]g / ml. The invention also provides a preparation method of the bibenzyl compounds.

Description

technical field [0001] The invention relates to a bibenzyl compound, a preparation method thereof and an application in the preparation of antitumor drugs. Background technique [0002] The existing literature reports that the following bibenzyl compounds have the efficacy and use of inhibiting passive cutaneous anaphylaxis and inhibiting the release of β-hexosaminidase from RBL-2H3 cells (basophilic leukemia cells) (See: Matsuda H et al. Antiallergic Phenanthrenes and... Planta Med 2004; 70:847-855): [0003] [0004] At present, there is no research report on the use of the bibenzyl compounds of the present invention for the preparation of antitumor drugs. Contents of the invention [0005] The purpose of the present invention is to provide a new application of the bibenzyl compounds as shown below, specifically the application in the preparation of drugs for treating and / or preventing tumors. [0006] Use of the compound represented by formula IV or its pharmaceuti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/085A61K31/09A61P35/00C07C41/34C07C41/36C07C41/38C07C43/23
CPCA61K31/085A61K31/09A61K36/898C07C41/34C07C41/36C07C41/38C07C43/23
Inventor 彭成戴鸥熊亮仰莲郭力
Owner CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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