3-hydrogenated pinicolic acid cyanide ethyl ester medicine and application thereof

A technology of cyanoethyl pine linate and ethyl acetate, which is used in drug combinations, steroids, antitumor drugs, etc.

Active Publication Date: 2016-09-21
CHINA THREE GORGES UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] 3-Hydropinemic acid cyanoethyl ester is an ester compound synthesized from the raw material of trihydropinemic acid B, and the defects of the prior art are the purification of trihydropinemic acid B and the purification of 3-hydropinolic acid B. separation and purification process

Method used

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  • 3-hydrogenated pinicolic acid cyanide ethyl ester medicine and application thereof
  • 3-hydrogenated pinicolic acid cyanide ethyl ester medicine and application thereof
  • 3-hydrogenated pinicolic acid cyanide ethyl ester medicine and application thereof

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Experimental program
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Effect test

Embodiment 1

[0056] 3-Hydropine acid cyanoethyl ester, its system name is: (2R)-2-((3S,10S,13R,14R,17R)-3-hydroxy-4,4,10,13,14-pentamethyl Base-2,3,4,5,6,7,10,11,12,13,14,15,16,17-tetrahydro-1H-cyclopenta[a]phenanthrene-17-yl)-6- Methylhept-5-enoic acid cyanomethyl ester; its structural formula is:

[0057]

[0058] The synthetic method of 3-hydropinine acid cyanoethyl ester is:

[0059] 1) Add equimolar 3-hydropinoseic acid B, bromoacetonitrile, and potassium carbonate into the reaction flask, and add an appropriate amount of acetonitrile as a solvent, stir and react at 85°C for 2 hours, after the reaction is detected by TCL, spin to dry the solvent, and add water and ethyl acetate, separated and extracted three times, reclaimed ethyl acetate to obtain a solid;

[0060] 2) Load the solid by the solid method, and separate it by 200-300 mesh normal phase silica gel column chromatography, using petroleum ether: ethyl acetate = 15:1 (volume ratio) as the mobile phase to obtain a white so...

Embodiment 2

[0065] One, on the basis of embodiment 1, the obtained 3-hydropinine acid cyanoethyl ester is carried out concrete experiment, concrete method is as follows:

[0066] 1. Cell culture

[0067] Human gastric cancer cell line HGC-27, human liver cancer cell line HepG2, human lung cancer cell line A549, human breast cancer cell line MDA-MB-231, human prostate cancer cell line PC3, and human nasopharyngeal cancer cell line CNE-2, respectively Cultured in RPMI-1640 medium containing 10% fetal bovine serum, neuroblastoma SH-SY5Y, and human colon cancer HT-29 cell line were cultured in DMEM medium containing 10% fetal bovine serum, placed at 37°C and 5% CO 2 Open monolayer cell culture was carried out in a saturated humidity incubator. When the cell density is about 80% observed under an inverted microscope, subculture is carried out. When subculture, first discard the old culture medium, then wash twice with 5mL PBS, add 0.25% trypsin, and store at 37°C, 5% CO 2 Incubate in the i...

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Abstract

The invention discloses a 3-hydrogenated pinicolic acid cyanide ethyl ester medicine and application thereof. The medicine comprises a compound with the following structure formula which is as shown in the description. The medicine also comprises pharmaceutically acceptable salts, 3-hydrogenated pinicolic acid cyanide ethyl ester as well as derivatives and pharmaceutically acceptable salts thereof, and pharmaceutically acceptable auxiliary materials or carriers. The 3-hydrogenated pinicolic acid cyanide ethyl ester is a PI3K / mTOR dual inhibitor; the invention also relates to application of the 3-hydrogenated pinicolic acid cyanide ethyl ester medicine to promotion of cell autophagy and application of the 3-hydrogenated pinicolic acid cyanide ethyl ester medicine to preparation of medicines for treating tumors such as gastric cancer, liver cancer, lung cancer, prostatic cancer and nasopharynx cancer and the like, neurodegenerative diseases such as presenile dementia and the like, and diabetes. The 3-hydrogenated pinicolic acid cyanide ethyl ester medicin provides a novel clinical medication choice.

Description

technical field [0001] The present invention relates to 3-hydropinate cyanoethyl ester drugs and applications thereof. As a PI3K / mTOR dual inhibitor, it can produce pharmacological effects on promoting cell autophagy, and 3-hydropine pinate cyanoethyl ester drugs can be used In the preparation of drugs for the treatment of gastric cancer and other cancers, Alzheimer's disease-like neurodegenerative diseases or diabetes. Background technique [0002] 3-Hydropinemic acid cyanoethyl ester is an ester compound synthesized from the raw material of trihydropinemic acid B, and the defect of the prior art is the purification of trihydropinemic acid B and 3-hydropinolic acid cyanoethyl ester separation and purification process. Contents of the invention [0003] The object of the present invention provides a kind of cyanoethyl 3-hydropinate and its application. [0004] In order to solve the above-mentioned technical problems, the technical scheme adopted in the present invention...

Claims

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Application Information

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IPC IPC(8): C07J9/00A61P35/00A61P25/28A61P3/10A61P43/00
CPCC07J9/005
Inventor 汪鋆植张盼闫喜明黄年玉余海立佘欣欣邓改改苟保灵贺海波李湜
Owner CHINA THREE GORGES UNIV
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