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Applications of catechin compounds

A technology of catechins and compounds, applied in the field of medicinal chemistry, can solve problems such as drug resistance and achieve good application prospects

Inactive Publication Date: 2017-09-01
SHANGHAI INST OF ORGANIC CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The technical problem to be solved by the present invention is to overcome the problem that the existing BCR-ABL inhibitors that have been used for tumor treatment have drug resistance, and provide a catechin compound used in the preparation of BCR-ABL kinase inhibitors. application

Method used

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  • Applications of catechin compounds
  • Applications of catechin compounds
  • Applications of catechin compounds

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0041] (1) Preparation of solution

[0042] ① Enzyme reaction buffer is 25mmol / L Tris, which contains 1mmol / L DTT, 100mmol / L NaCl, 10mmol / L MgCl 2 , and use H 3 PO 4 Adjust the pH to 7.5.

[0043] ②Use 2 μL enzyme reaction buffer to dissolve the substrate peptide (containing 1×10 -7 mol / L sodium fluorescein as an internal standard to improve the accuracy of quantification) and BCR-ABL, wherein the concentration of the substrate peptide is 10 μmol / L, and the concentration of BCR-ABL is 2 μg / mL.

[0044] (2) Experimental process

[0045] In this example, BCR-ABL was reacted with a substrate peptide, and the inhibitory activity of epicatechin gallate on this reaction was examined.

[0046] In this example, capillary electrophoresis (CE) was used to separate the reaction system of 2 μg / mL BCR-ABL and 10 μmol / L BCR-ABL substrate peptide, and the absence of catechin compounds (that is, the addition of 0.25% dimethyl The difference of the reaction system after adding catechin c...

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Abstract

The invention discloses applications of catechin compounds shown in the formula I in the specification or a stereoisomer, a tautomer, pharmaceutically acceptable salt, solvate, metabolite or prodrugs in preparation of BCR-ABL kinase inhibitors and in preparation of medicines for treating BCR-ABL kinase activated and mediated diseases. The BCR-ABL kinase activated and mediated diseases are proliferative diseases. The catechin compounds can effectively inhibit the catalytic activity of BCR-ABL enzymes and have better application prospects in preparation of medicines for treating the BCR-ABL kinase activated and mediated diseases.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to the application of catechin compounds. Background technique [0002] Breakpoint clustered region-Abelson protein (BCR-ABL) is a non-receptor tyrosine protein kinase. The normal ABL gene is on chromosome 9 and the BCR gene is on chromosome 22. Chromosome 9 and chromosome 22 translocate to each other to form the Philadelphia chromosome (Ph). The repressive region at the N-terminal of the ABL gene in the Philadelphia chromosome is eliminated, thus encoding the BCR-ABL kinase that is in a continuously active state, causing cell proliferation and adhesion. And changes in the nature of survival, resulting in chronic myeloid leukemia (CML) and acute myeloid leukemia (ALL). [0003] Imatinib (Gleevec, Novartis) is the first BCR-ABL kinase inhibitor approved for marketing, and it is also the first small molecule kinase inhibitor. Although imatinib has achieved great succe...

Claims

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Application Information

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IPC IPC(8): A61K31/353A61P35/00A61P35/02
CPCA61K31/353
Inventor 康经武徐美
Owner SHANGHAI INST OF ORGANIC CHEM CHINESE ACAD OF SCI