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Coupled peptide compound as protein tyrosine kinase inhibitor

A peptide compound and compound technology, applied in the field of chemistry, can solve problems such as unsatisfied, and achieve the effects of high safety, good inhibitory activity, and broad market prospects

Active Publication Date: 2015-10-14
深圳市康尔诺生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, improvements (such as high-affinity and and / or alternative) molecules, there is still an unmet need

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The preparation of embodiment 1 peptidyl substitution compound

[0027] (1) [5-[[(2,4,6-trimethylphenyl)amino]carbonyl]-4-methyl-2-thiazolyl]carbamate, 1,1-dimethylethyl ester (10 g, 26.63 mmol) in trifluoroacetic acid (100 mL) was stirred at room temperature for 3 hours. The solution was concentrated under reduced pressure, the residue was diluted with ethyl acetate (700 mL) and washed with 5% KHCO 3 Aqueous (400 mL, 2x), water and brine washes; dried (MgSO 4 ), filtered and concentrated. The residue was washed with diethyl ether (200 mL) and acetonitrile (100 mL) to give compound S1 as a white solid;

[0028] (2) Alkylation reaction of S1 with chloroacetic acid in an alkaline environment, and then chlorination reaction with thionyl chloride to obtain compound S2 or the substitution of Cl by other methods commonly used in the field;

[0029] (3) Substituting S2 with glycine to obtain compound S3;

[0030] (4) Link the compound of S3 with different amino acids (GTH...

Embodiment 2

[0031] Example 2 Functional Verification of Peptidyl Substituted Compounds

[0032] Human lung adenocarcinoma cell line A549 was cultured in RPMI1640 medium (containing 10% inactivated calf serum, 100 U / mL penicillin and 100 U / mL streptomycin) and grown in a 37 °C, 5% CO2 incubator.

[0033] Digest and prepare cell suspension at 1×105 / mL, add 100 μL of cell suspension to each well of a 96-well plate, and culture for 24 h to adhere to the wall. The medium was changed, and culture medium containing different concentrations of drugs was added, 100 μL per well, 4 parallel wells were set for each concentration, and the final concentration of the compound was 2.0 mg / L. Continue to cultivate for 72 h. Add 20 μL MTT (5 mg / mL) to each well, return to the incubator, and continue to incubate for 4 h. Discard the supernatant, add 150 μL DMSO to each well, shake slightly for 15 min to fully dissolve the crystals, set the blank control well to zero, select a wavelength of 490 nm within 20...

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PUM

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Abstract

The invention relates to a coupled peptide compound as a protein tyrosine kinase inhibitor. The coupled peptide compound is shown in the formula (I). The coupled peptide compound can be used for treating one or more protein tyrosine kinase-mediated diseases.

Description

technical field [0001] The invention belongs to the field of chemistry, in particular, the invention relates to anticancer compounds. Background technique [0002] Protein kinases (PKs) are enzymes that catalyze the phosphorylation of specific serine, threonine or tyrosine residues in cellular proteins. Post-translational modifications of these substrate proteins act as molecular switches that regulate cell proliferation, activation and / or differentiation. Aberrant or excessive PK activity has been observed in many disease states including benign and malignant proliferative disorders. In many cases it has been feasible to use PK inhibitors to treat diseases such as proliferative diseases in vitro, and in many cases it has been feasible to use PK inhibitors to treat diseases such as proliferative diseases in vivo. The kinases are mainly divided into two groups: those that specifically phosphorylate serine and threonine and those that specifically phosphorylate tyrosine. In...

Claims

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Application Information

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IPC IPC(8): C07K5/08C07K5/10C07K1/06A61K38/06A61K38/07A61P35/00
Inventor 杨洋
Owner 深圳市康尔诺生物技术有限公司
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