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Application of RhoGDI inhibitor to preparation of drugs for treating nasopharynx cancer

An inhibitor and nasopharyngeal carcinoma technology, applied in the field of application of RhoGDI inhibitors in the preparation of drugs for the treatment of nasopharyngeal carcinoma, can solve the problems of inability to achieve effectiveness and achieve good clinical application prospects

Active Publication Date: 2018-05-08
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Targeted drugs that have been clinically studied in nasopharyngeal carcinoma mainly include EGFR inhibitors nimotuzumab, cetuximab, gefitinib and angiogenesis inhibitors bevacizumab, sunitinib, Pazopanib, most of these drugs are in phase II exploratory studies and cannot meet the expected effectiveness of clinical trials

Method used

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  • Application of RhoGDI inhibitor to preparation of drugs for treating nasopharynx cancer
  • Application of RhoGDI inhibitor to preparation of drugs for treating nasopharynx cancer
  • Application of RhoGDI inhibitor to preparation of drugs for treating nasopharynx cancer

Examples

Experimental program
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Effect test

preparation example Construction

[0036] Preparation of compound 3:

[0037] Weigh successively 10.0g benzylamine (compound 1), 19.3g K 2 CO 3 In 150ml of dichloromethane, stir. Then 12.7 g of chloroacetyl chloride (compound 2) was weighed and added dropwise to the mixture at room temperature. After the dropwise addition, the mixed system was heated to reflux and reacted for 6h. Cool down to room temperature, and slowly add 200ml of ice water with stirring. After standing still for 5 minutes, separate the liquids, extract the aqueous phase twice with 100ml of dichloromethane, combine the organic phases, wash with 20ml of saturated brine, dry over anhydrous sodium sulfate, filter, concentrate to dryness, and purify by column chromatography to obtain 12.1g Compound 3, yield 71.1%.

[0038] Preparation of Compound 5:

[0039] Weigh 9.9g of compound 4 in 100ml of acetone, then add 15.0g of potassium carbonate and stir. 10 g of compound 3 was dissolved in 50 ml of acetone, and added dropwise to the mixture a...

Embodiment 1

[0045] Embodiment 1, compound SKLB-163 of the present invention treats nasopharyngeal carcinoma

[0046] 1 experimental reagent

[0047] MTT (dimethylthiazolediphenyltetrazolium bromide): available from Sigma Chemical

[0048] DMSO (dimethyl sulfoxide): purchased from Sigma Chem

[0049] Crystal violet, puromycin: purchased from Sigma-Aldrich

[0050] DMEM, fetal bovine serum, trypsin: purchased from GIBGO BRL company

[0051] Protein Assay Kit: purchased from Bio-Rad

[0052] Acrylamide: purchased from Bio-Rad

[0053] RhoGDI, p-JNK-1 (Thr183 / Tyr185), p-AKT (Ser473) primary antibodies: purchased from Cell Signaling Technology

[0054] p-c-Jun(Tyr170), caspase-3, GAPDH primary antibodies: purchased from Santa Cruz Biotechnology, USA

[0055] PVDF membrane: purchased from Millipore

[0056] In situ TUNEL detection kit: purchased from Promega

[0057] PCNA antibody: purchased from Cell Signaling Technology

[0058] Horseradish peroxide-labeled goat anti-rabbit IgG and g...

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PUM

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Abstract

The invention discloses application of a RhoGDI inhibitor to the preparation of drugs for treating nasopharynx cancer. The invention further discloses application of a RhoGDI inhibitor to the preparation of nasopharynx cancer radiotherapy sensitizer. The invention further discloses a drug for treating nasopharynx cancer, which adopts a preparation prepared from the RhoGDI inhibitor taken as an active component and pharmaceutically acceptable auxiliary materials. The RhoGDI inhibitor achieves the effects of tumor growth resistance, tumor metastasis resistance and radiotherapy sensitivity through specific inhibition of RhoGDI expression and activation of a JNK-1 pathway at the downstream (namely the activation of the expression of downstream p-JNK-1, c-Jun, inhibition the expression of p-AKT, enhancement the conversion of pro-caspase-3 to cleaved-caspase-3), and has a good clinical application prospect.

Description

technical field [0001] The invention relates to the application of RhoGDI inhibitor in the preparation of medicine for treating nasopharyngeal carcinoma. Background technique [0002] Nasopharyngeal carcinoma refers to malignant tumors that occur on the roof and side walls of the nasopharyngeal cavity. It is one of the high-incidence malignant tumors in my country, and its incidence rate is the first among ear, nose and throat malignant tumors. Common clinical symptoms are nasal congestion, blood in the nasal discharge, ear blockage, hearing loss, diplopia, and headache. [0003] At present, radiotherapy is the main effective treatment for nasopharyngeal carcinoma, but for locally advanced nasopharyngeal carcinoma, the combination of radiotherapy and chemotherapy has gradually become the standard mode. The development of radiotherapy techniques and the improvement of chemotherapy regimens have greatly improved the local control rate of NPC patients, but the long-term survi...

Claims

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Application Information

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IPC IPC(8): A61K31/428C07D277/74A61P35/00
CPCC07D277/74
Inventor 彭星辰何金兰李平
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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