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c-Myc gene expression inhibitor and application thereof

A gene expression, c-myc technology, applied in medical preparations containing active ingredients, organic active ingredients, drug combinations, etc. Toxicity, inducing tumor cell apoptosis, and inhibiting growth

Active Publication Date: 2019-05-31
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, so far, humans have not successfully developed clinical anti-tumor drugs targeting the c-Myc gene

Method used

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  • c-Myc gene expression inhibitor and application thereof
  • c-Myc gene expression inhibitor and application thereof
  • c-Myc gene expression inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Embodiment 1: the preparation of compound PA1

[0053] The main synthesis steps: activate the resin, remove the protective group on the resin, activate the carboxyl group, couple, cap, cut the resin and other parts.

[0054] Activation of the resin: fully swell the resin with DMF.

[0055] Deprotection: Deprotect the Fmoc protecting group from the Fmoc-protected resin by piperidine / DMF solution to release the free amino group.

[0056] Activation of the carboxyl group: The carboxyl group of the amino acid involved in the next coupling reaction is activated by the activation reagent HBTU to form an activated ester, thereby efficiently coupling with the amino group.

[0057] Coupling: Activated amino acids react with free amino groups on the resin to form peptide bonds.

[0058] Capping: There are some incompletely reacted amino structures in the reaction, which must be capped to avoid side reactions in the next coupling, so as to ensure the purity of the synthesized ta...

Embodiment 2

[0092] Embodiment 2: the preparation of compound PA2

[0093] The synthesis steps are similar to the synthesis of PA1( Figure 3A ). Proceed as follows:

[0094] 1) Activation: same as the first step 1) activation of PA 1 preparation. weigh Figure 3B Fmoc protection β-alanine-Clear resin (SPS-1, 1.00g, 0.4mmol, Peptides International) as shown in formula (12) joins in the solid-phase reaction tube of solid-phase reaction device, logical nitrogen protection, again Add 5mL of DMF to fully bubble nitrogen for 30min to activate the resin;

[0095] 2) Deprotection: first prepare 3 mL of 20% (v / v) piperidine / DMF (both piperidine and DMF are treated anhydrous solvents), and add it to the solid-phase reaction tube of step 1) under nitrogen protection, Fully bubbling reaction for 15 minutes, remove the amino protecting group on β-alanine, remove the solvent in the reaction tube, rinse twice with 3mL anhydrous dichloromethane, rinse once with 2mL anhydrous DMF, each time Drain th...

Embodiment 3

[0119] Embodiment 3: the preparation of compound PA3

[0120] The synthesis steps are similar to the synthesis of PA1( Figure 3A ). Proceed as follows:

[0121] 1) Activation: same as the first step 1) activation of PA 1 preparation. weigh Figure 3B Fmoc protection β-alanine-Clear resin (SPS-1, 1.00g, 0.4mmol, Peptides International) as shown in formula (12) joins in the solid-phase reaction tube of solid-phase reaction device, logical nitrogen protection, again Add 5mL of DMF to fully bubble nitrogen for 30min to activate the resin;

[0122] 2) Deprotection: first prepare 3 mL of 20% (v / v) piperidine / DMF (both piperidine and DMF are treated anhydrous solvents), and add it to the solid-phase reaction tube of step 1) under nitrogen protection, Fully bubbling reaction for 15 minutes, remove the amino protecting group on β-alanine, remove the solvent in the reaction tube, rinse twice with 3mL anhydrous dichloromethane, rinse once with 2mL anhydrous DMF, each time Drain th...

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Abstract

The invention discloses a c-Myc gene expression inhibitor, and application thereof to preparing anti-tumor medicines. The c-Myc gene expression inhibitor is a pyrrole-imidazole polyamide small molecule. The pyrrole-imidazole polyamide small molecule is targeted to a c-Myc gene promoter sequence through a recognizing and pairing mode, and the expression of a c-Myc gene is silenced. Polyamide PA6 presents good tumor cytotoxicity, the growth of tumor cells can be restrained, and the apoptosis of the tumor cells is induced.

Description

technical field [0001] The invention relates to a c-Myc gene expression inhibitor and application thereof. Background technique [0002] Polyamides are generally composed of 2-3 different five-membered aromatic heterocycles: N-methylpyrrole (Py, aromatic residue), N-methylimidazole (Im, aromatic residue) and 3-hydroxy-N-formazol Composition of pyrrole (Hp, aromatic residue); in the DNA minor groove, two polyamides or hairpin polyamides are antiparallel, side by side with the predetermined DNA base sequence at a ratio of 1:1 to closely and specifically recognize bases The synthetic small molecule compound of the synthetic small molecular compound, namely N-methylpyrrole (Py) tends to recognize T, A and C base; N-methylimidazole (Im) is the reading element of G base; 3-hydroxyl-N-methyl The base pyrrole (Hp) can specifically recognize the T base. So far, Im / Py and Py / Im pairings recognize G·C and C·G respectively, while Hp / Py pairing can distinguish base pairs T·A and A·T. ...

Claims

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Application Information

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IPC IPC(8): A61K31/787A61P35/00
Inventor 张文付伟吴艳玲陈冰佳陈兴来
Owner ZHEJIANG UNIV OF TECH
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