Application of aromatic alkanoyl tetrahydro-beta-carboline and derivative thereof in treatment of cancer

A technology of aryl alkanoyl tetrahydro and aryl, which is applied in the field of related diseases, can solve the problems of unsatisfactory physical and chemical properties of compounds, restrictions on the research of compound druggability, and unclear molecular mechanism of action of compounds, etc., to achieve improvement of pharmacokinetic properties , Excellent therapeutic effect

Active Publication Date: 2013-03-20
EAST CHINA NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, compounds containing this type of structure usually have several obvious shortcomings. First, the molecular mechanism of action of the compound is not clear enough, so the research on its pharmacological effect is relatively lacking; in addition, another defect of this type of compound is that the physical and chemical properties of the compound are not enough. ideal, which largely limits druggability studies of such compounds

Method used

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  • Application of aromatic alkanoyl tetrahydro-beta-carboline and derivative thereof in treatment of cancer
  • Application of aromatic alkanoyl tetrahydro-beta-carboline and derivative thereof in treatment of cancer
  • Application of aromatic alkanoyl tetrahydro-beta-carboline and derivative thereof in treatment of cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0117] Embodiment one: the preparation of each compound

Embodiment 1-1

[0118] Example 1-1, Synthesis of N-phenylacetyl-(6-trifluoromethyl)-1,3,4,9-tetrahydro-1H-β-carboline (NTC001)

[0119]Take 4-trifluoromethylphenylhydrazine hydrochloride (425mg, 2mmol) in 14mL alcohol and water (volume ratio is 5 / 1), slowly add 4-chlorobutyraldehyde dimethyl acetal (367mg, 2.2 mmol), then warming and flowing for 5-18 hours. Complete, remove most of the solvent under reduced pressure, then adjust the pH value of the solution to 12, extract three times with ethyl acetate, combine the organic phases, dry with anhydrous sodium sulfate, and distill off the solvent under reduced pressure to obtain the intermediate 5-trifluoroform Tritryptamine (crude product 464mg).

[0120] 5-Trifluoromethyltryptamine (464mg, 2.0mmol) was dissolved in 3mL of glacial acetic acid, and 37% formaldehyde solution (45μL, 0.60mmol) was added dropwise under the protection of nitrogen to complete the addition and react overnight. Most of the acetic acid was evaporated under reduced press...

Embodiment 2-52

[0122] Preparation of NTC002-52 carboline compounds shown in Example 2-52 and Table 1 (see reference below for specific process)

[0123]

[0124]

[0125]

[0126]

[0127]

[0128]

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PUM

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Abstract

The present invention discloses an aromatic alkanoyl tetrahydro-beta-carboline compound represented by a structural formula (I), and related analogs thereof or hydrates or pharmaceutically acceptable salts thereof, and the application of the compound or pharmaceutical compositions containing the compound in the preparation of drugs for treatment of various cancers and tumor metastasis.

Description

technical field [0001] The present invention relates to a compound represented by the following structure (I) and related derivatives, and the use of the compound or the pharmaceutical composition containing the compound for treating various malignant tumor growth and tumor metastasis and other related diseases. Background technique [0002] Malignant tumor is one of the major diseases faced by human beings. With the rapid development of my country's economy, changes in lifestyles, increasing pressure on survival, aggravated population aging problems and deepening urbanization, the occurrence and development of malignant tumors have become an important obstacle to the further improvement of people's quality of life, and pose a serious threat to individuals and society. Bring heavy economic and spiritual burden. Around the world, about 6.9 million people die from malignant tumors every year, and about 8.7 million new cases occur. It is estimated that 12 million people will di...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04A61K31/437A61K31/5377A61K31/496A61P35/00A61P35/04A61P35/02
Inventor 刘明耀陈益华罗剑周文波秦敏易正芳
Owner EAST CHINA NORMAL UNIV
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