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Compound with heat shock heat protein 70 inhibitory activity and application thereof

A heat shock protein and inhibitory activity technology, which is applied in the field of compounds with heat shock protein 70 inhibitory activity, can solve the problems of weak GSH reactivity and achieve the effect of low side effects and high activity

Active Publication Date: 2021-07-09
PEKING UNIV SHENZHEN GRADUATE SCHOOL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

PES can selectively kill tumor cells, but has no toxicity to normal cells at the same concentration, and can inhibit the activity of tumor cells such as leukemia, lymphoma, bladder cancer, pancreatic cancer, non-small cell lung cancer, and cervical cancer. Glutathione (GSH), which exists in large quantities in the body, also has strong responsiveness, so it is necessary to develop inhibitors that have weak responsiveness to GSH and maintain or improve the binding ability to Hsp70, so as to improve the activity of compounds in complex biological systems and reduce possible side effects

Method used

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  • Compound with heat shock heat protein 70 inhibitory activity and application thereof
  • Compound with heat shock heat protein 70 inhibitory activity and application thereof
  • Compound with heat shock heat protein 70 inhibitory activity and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] A compound with heat shock protein 70 inhibitory activity, the chemical structural formula of the compound is as follows:

[0022]

[0023] The compound of this example is prepared by the route of the above reaction formula.

Embodiment 2

[0025] A compound with heat shock protein 70 inhibitory activity, the chemical structural formula of the compound is as follows:

[0026]

[0027] The compound of this example is prepared by the route of the above reaction formula.

Embodiment 3

[0029] A compound with heat shock protein 70 inhibitory activity, the chemical structural formula of the compound is as follows:

[0030]

[0031] The compound of this example is prepared by the route of the above reaction formula.

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Abstract

The invention belongs to the technical field of medicines, and particularly provides a compound with heat shock protein 70 inhibitory activity and application thereof. The compound comprises at least one of three compounds in the specification. The compound provided by the invention has weak reaction capacity to glutathione and strong binding capacity to heat shock protein 70, and has high activity and low side effect in a complex biological system, so that the compound can be used as an inhibitor.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a compound with heat shock protein 70 inhibitory activity and application thereof. Background technique [0002] Heat shock protein 70 (Hsp70) is widely distributed in various organisms, and its sequence and structure are highly conserved from lower bacteria to higher mammals. Hsp70 consists of an amino-terminal nucleotide-binding domain, a carboxy-terminal substrate-binding domain (SBD), and a hydrophobic flexible chain of about ten amino acid residues connecting between the nucleotide-binding domain and the substrate-binding domain. Among them, the substrate-binding domain (SBD) can be further divided into β-sheet-rich SBDβ subdomain and α-helix-rich SBDα subdomain. [0003] There are literature reports, (PES) is an inhibitor of Hsp70 and is thought to possibly bind to the SBD of Hsp70. PES can selectively kill tumor cells, but has no toxicity to normal cells at the same c...

Claims

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Application Information

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IPC IPC(8): C07D213/34C07D295/26C07C311/13A61P35/00A61K31/4406A61K31/40A61K31/18
CPCC07D213/34C07D295/26C07C311/13A61P35/00Y02A50/30
Inventor 潘峥婴杨杰
Owner PEKING UNIV SHENZHEN GRADUATE SCHOOL
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