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Application of N-[4-(N-{5-[(2,3-dihydro-1H-indene-5-yloxy) methyl]-2-furyl}acethydrazide)phenyl]cyclopentane formamide in preparing anti-tumor medication

A technology of cyclopentanecarboxamide and anti-tumor drugs, which is applied to the application field of compounds in the preparation of anti-tumor drugs, can solve problems such as adverse reactions of anti-tumor drugs, and achieve the effects of being less resistant to drug resistance, inhibiting proliferation and having obvious effects.

Inactive Publication Date: 2010-09-29
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Malignant tumors have become one of the most important causes of human death, but currently available anti-tumor drugs have various adverse reactions. Therefore, finding new anti-tumor drugs with low side effects has become a hot spot in the field of biomedicine

Method used

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  • Application of N-[4-(N-{5-[(2,3-dihydro-1H-indene-5-yloxy) methyl]-2-furyl}acethydrazide)phenyl]cyclopentane formamide in preparing anti-tumor medication

Examples

Experimental program
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Effect test

Embodiment 1

[0023] Example 1 Proves the ability of small molecule compounds to inhibit CypA enzyme activity by using enzyme activity experiments

[0024] There are many methods for measuring CyP activity, but α-chymotrypsin-coupled enzymic assay is the most commonly used.

[0025] We took the reaction without small molecule inhibitors as the control reaction, measured the inhibition rate of each small molecule ligand on the enzyme activity reaction at different concentrations, and calculated the IC of each small molecule ligand 50 value. N-[4-(N-{5-[(2,3-dihydro-1H-inden-5-yloxy)methyl]-2-furyl}acetylhydrazino)phenyl]cyclopentyl of the present invention Alkanecarboxamides (CHEMCATS Order Number: AK-968 / 15604391). Its enzyme activity inhibition IC 50 The value (μM) was 18.67±1.74.

Embodiment 2

[0026] Embodiment 2MTS method measures the growth inhibitory effect of FD068 on SK-Hep1 cells

[0027] Human liver cancer cell line SK-Hep1 cells (ATCC company) 2~5×10 3 Each well was inoculated into a 96-well plate, cultured for 24 hours to allow it to adhere to the wall, and then FD068 (Interchim, AK-968 / 15603640) was added to set up 6 concentration gradients and 3 replicate wells for each concentration. Cells at 37°C, 5% CO 2After culturing for 72 hours under the same conditions, discard the culture medium, and use the MTS kit (Promega Company) to measure the cell survival rate. The test method is as follows: wash the cells once with serum-free medium, and add the pre-prepared MTS chromogenic solution (add 2 ml of solution 1 and 100 μl of solution 2 to 10 ml of serum-free medium, and mix thoroughly). A well without cells was set as the background well to correct for the background light absorption of the solution. Put the cells into the cell incubator and continue to cul...

Embodiment 3

[0030] Effect of embodiment 3FD068 on clone formation rate

[0031] 1000 cells / dish of SK-Hep1 cells (ATCC Company) were inoculated on 60 mm cell culture dishes, one group was added with FD068, and the other group was added with DMSO as a control. Continuously cultivate for 15-20 days, and change the medium as appropriate in the middle. Wash once with room temperature 1×PBS, add 2ml of pre-cooled methanol and fix at 4°C for 10min. Discard the methanol used for fixation, wash once with pre-cooled 1×PBS, add GIMESA stain, stain at room temperature for 10 min, wash 3 times with water, remove floating color, take pictures, and count.

[0032] The clone size is determined according to the number of cells. Those larger than 200 cells are called large clones, those between 100-200 cells are called medium clones, and those between 50-100 cells are called small clones. Compare the difference between large and medium clones, repeat twice and take the average value of three dishes each...

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Abstract

The invention belongs to the field of gene engineering and chemistry and relates to application of N-[4-(N-{5-[(2,3-dihydro-1H-indene-5-yloxy) methyl]-2-furyl}acethydrazide)phenyl]cyclopentane formamide in preparing an anti-tumor medication. Search of a novel anti-tumor medication with little side effect is a large hot spot in the biomedical field. The N-[4-(N-{5-[(2,3-dihydro-1H-indene-5-yloxy) methyl]-2-furyl}acethydrazide)phenyl]cyclopentane formamide can obviously inhibit proliferation of tumor cells, is designed aiming to a cell target CYPJ protein structure and has specially obvious effect on high expression of CYPJ protein of tumor cells. Therefore, the micromolecule compound is developed as a new anti-tumor medication and has obvious tumor inhibition effect and favorable specificity.

Description

technical field [0001] The invention relates to the fields of chemical industry and medicine, and relates to the application of a compound in the preparation of antitumor drugs. Background technique [0002] Cycliphilins (CyPs) are ubiquitously distributed intracellular proteins that are highly conserved in plants, bacteria, and mammals. They were originally discovered as cellular receptors for cyclosporin A. Cyclosporin A (Cyclosporin A, CsA) is a cyclic polypeptide containing 11 amino acids isolated from fungal metabolites. It is an immunosuppressant for organ transplantation and autoimmune diseases, and has been widely used clinically. , with annual sales of more than 5 billion US dollars. Since CsA has shown various toxic and side effects since it was used in clinical practice, people pay more and more attention to its impact on the survival rate of patients and grafts. Many scientific researchers are trying to find alternatives with similar effects to CsA and low toxic...

Claims

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Application Information

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IPC IPC(8): A61K31/341A61P35/00A61P1/16
Inventor 余龙张明君
Owner FUDAN UNIV
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