Bibenzyl compound, preparation method thereof and use thereof in preparation of antitumor drugs

A technology for compounds and solvates, applied in the field of anti-tumor drug preparation, can solve the problems of no anti-tumor drug research report, no compound research report, etc., and achieves high yield, simple preparation method, and convenient operation and control. Effect

Inactive Publication Date: 2017-01-25
CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patented novel chemicals have been found effective against certain types of cancers like lung or colon carcinoma cell lines that are resistant to other treatments such as chemotherapy drugs. They also produce less harmful side-effects compared with current methods used at home (such as surgery). These technical results make them ideal candidates for use in industry.

Problems solved by technology

This patented technical problem addressed in this patents relates to finding new ways to prevent or treat skin cancer caused by exposure to harmful chemicals such as ultraviolet light.

Method used

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  • Bibenzyl compound, preparation method thereof and use thereof in preparation of antitumor drugs
  • Bibenzyl compound, preparation method thereof and use thereof in preparation of antitumor drugs
  • Bibenzyl compound, preparation method thereof and use thereof in preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0092] Example 1, the extraction and structural identification of compound D

[0093] (1) Extraction of medicinal materials:

[0094] Dried white and medicinal material coarse powder (3kg), reflux extraction with 95% ethanol 3 times (30L×3), 2h each time;

[0095] (2) Separation and purification of components:

[0096] 1. Ethanol extract (90L) was concentrated and dried under reduced pressure to obtain 510g of semi-solid liquid extract;

[0097] 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;

[0098] 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;

[0099] The c...

Embodiment 2

[0116] Example 2, the extraction and structural identification of compound E

[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...

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PUM

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Abstract

The invention discloses a compound represented by a formula III (shown in the description) or pharmaceutically acceptable salt, crystal forms and solvates thereof. According to the compound, R1 and R2 are respectively independently selected from hydroxyl group or sulfydryl or halogen-substituted C1-C4 alkyl; and R3, R4 and R5 are respectively independently selected from hydroxyl group or sulfydryl. The novel compound represented by the formula III has a very good inhibiting effect to tumor cells and particularly has a very good inhibiting effect to lung cancer cells, and IC50 thereof reaches 4-5 microgram/microliter; and meanwhile, the preparation method of the compound is simple and convenient, reaction conditions are mild, the operation and the control are convenient, the energy consumption is low, the yield is high, the cost is low, and the preparation method is very suitable for industrial production.

Description

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Claims

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Application Information

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Owner CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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