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HDAC6 selective inhibitor

A selective and inhibitory technology, applied in the field of anti-tumor drugs, can solve problems such as strong toxic and side effects, and achieve the effect of high inhibition rate

Active Publication Date: 2019-10-01
PEOPLES HOSPITAL OF HENAN PROV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Among them, SAHA and Panobinostat are non-selective HDACs inhibitors, which have strong toxic and side effects due to their inhibitory effect on many signaling pathways

Method used

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  • HDAC6 selective inhibitor
  • HDAC6 selective inhibitor
  • HDAC6 selective inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1 HDACs inhibitory activity

[0054] Inhibitory activity of G1 and G10 compounds on HDAC6: Compound G1 or G10 at a concentration of 20 μM was incubated with recombinant HDAC6 (BPS Biosciences, US) for 15 minutes at room temperature, and then the substrate Ac-peptide-AMC (7-amino-4- Coumarin-labeled acetylated peptide, Jill Biochemical) started the reaction. The reaction was carried out at room temperature for 60 minutes, then a trypsin solution was added to stop the reaction, and the reaction solution was stored at 37° C. for another 90 minutes. The fluorophore AMC released from the substrate was measured with Synergy2 (Biotek, US, excitation=355nm, emission=460nm). ,

[0055] Use Synergy to select the linear response segment to obtain the slope (slope). Then calculate the percentage inhibition rate, the calculation formula is as follows:

[0056]

[0057] Among them: Inhibition is the inhibition rate; Sample Signal is the slope of the compound hole; Mean...

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PUM

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Abstract

The invention relates to an HDAC6 selective inhibitor, and belongs to the technical field of medicine. The to-be-achieved technical purpose is to provide the novel HDAC6 selective inhibitor. The HDAC6selective inhibitor comprises a compound shown in a formula I and a pharmaceutically acceptable auxiliary material. It is found for the first time that the compound shown in the formula I can inhibitHDAC6 while having a small inhibitory effect on HDAC1 and HDAC10, therefore, the HDAC6 selective inhibitor can be prepared, the inhibition rate of the HDAC6 selective inhibitor is high, and a new choice is provided for the HDAC6 inhibitor.

Description

technical field [0001] The invention relates to a selective HDAC6 inhibitor, which belongs to the technical field of antitumor drugs. Background technique [0002] Histone deacetylases (HDACs) remove acetyl groups from ε-N-acetylated lysine residues in a variety of histone or other protein substrates. HDAC belongs to the evolutionary conservative family and can be divided into four categories: Classes I (HDAC1,2,3,8), IIa (HDAC 4,5,7,9), IIb (HDAC 6,10) and IV (HDAC 11 ) is a zinc-dependent enzyme, and Class III HDACs (sirtuins) are NAD-dependent enzymes. Among them, HDAC6 is mainly located in the cytoplasm, and may regulate the functions of many tumor-associated proteins through its deacetylase pathway. HDAC6 plays an important role in the formation of cell motility and invasiveness, and is an attractive target for the treatment of various tumors and neurodegenerative diseases. It is of great value to study selective HDAC6 inhibitors. [0003] At present, known histone d...

Claims

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Application Information

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IPC IPC(8): C07D471/04A61K31/437A61K31/444A61P35/00A61P25/00
CPCA61P25/00A61P35/00C07D471/04
Inventor 李德宇闫国毅李冬筱陶连元
Owner PEOPLES HOSPITAL OF HENAN PROV
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