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New application of aminoquinol

A technology with new use and effect, applied in the new use field of Rafoxanide, can solve the problems of strong side effects of anti-cancer chemotherapy drugs and no good anti-skin cancer chemotherapy drugs, so as to shorten the time of drug development, shorten the cost of clinical trials, save Cost and Time Effects

Inactive Publication Date: 2016-06-22
KUNMING MEDICAL UNIVERSITY +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

CDK4,6 is a key regulatory factor in the early stage of the G1 phase of the cell cycle. Inhibiting the cyclin-dependent kinase CDK4,6 can inhibit the proliferation of tumor cells and is a good tumor drug target. Drugs with the activity of sex kinase CDK4, 6 can inhibit the proliferation of tumor cells and exert the effect of anti-skin cancer; there are no good anti-skin cancer chemotherapy drugs clinically, and the clinical anti-cancer chemotherapy drugs have strong side effects, so the current clinical Chemotherapy drugs used on the skin are very limited in use, so it is imminent to find new and good anti-skin cancer drugs

Method used

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  • New application of aminoquinol
  • New application of aminoquinol
  • New application of aminoquinol

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Embodiment Construction

[0028] The technical solution of this patent will be further described in detail below in conjunction with specific embodiments.

[0029] A new application of Rafoxanide. The Rafoxanide is a target CDK4 / 6 inhibitor and has an anti-skin cancer effect. Rafoxanide is used to prepare an anticancer drug for treating skin cancer.

[0030] The definitive experiment for this new use included the following steps:

[0031] 1) Use computer idock software to screen out candidate CDK4 / 6 inhibitors against skin cancer targeting CDK4 / 6:

[0032] Analyzed 4,914 drugs from the FDA-certified ZINC drug database included in the dbap and fda catalogs and sorted them according to the binding affinity value, and found and purchased 9 compounds with the highest scores for the next step of the experiment; They are Lifibrate, Nizofenone, fumarate, Chloracyzine, adafenoxate, Cloricromene, Sulconazole, nitrate, Rafoxanide;

[0033] 2) Verify the candidate inhibitors screened in the first step through i...

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Abstract

The invention discloses a new application of Rafoxanide. The influence of Rafoxanide to the skin cancer cell lines A375 and A431 is tested through a series of experiments, and the experiments indicate that the Rafoxanide is a target CDK4 / 6 inhibitor and can increase the number of cells of A375 and A431 stagnating in the G1 stage and reduce the number of the cells in the S stage; the apoptosis rate of A375 and A431 can be increased; the protein expression of the CDK 4 / 6, cyclinD and pho-CDK4 / 6 of the signal channel in the G1 stage of a cell cycle can be inhibited, a skin cancer-resistant effect is realized, and thus, the Rafoxanide can be used for preparing anti-cancer medicines for treating skin cancer; and since the Rafoxanide is a medicine resisting parasitic diseases already registered by FDA, the later clinical experiment cost is reduced, the medicine development time is shortened, and the cost and time for developing a new anti-cancer medicine are greatly saved.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a new application of Rafoxanide. Background technique [0002] Cell cycle disorder is a sign of malignant tumor formation. The activation and inactivation of cyclin-dependent kinases (CDKs) maintain the orderly progress of each phase of the cell cycle. CDK4,6 is a key regulatory factor in the early stage of the G1 phase of the cell cycle. Inhibiting the cyclin-dependent kinase CDK4,6 can inhibit the proliferation of tumor cells and is a good tumor drug target. Drugs with the activity of sex kinase CDK4, 6 can inhibit the proliferation of tumor cells and exert the effect of anti-skin cancer; there are no good anti-skin cancer chemotherapy drugs clinically, and the clinical anti-cancer chemotherapy drugs have strong side effects, so the current clinical The chemotherapy drugs used on the skin are very limited in use, so it is extremely urgent to find new and good anti-skin cancer drugs. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/167A61P35/00
CPCA61K31/167
Inventor 石西南孔祥复李宏健梁广锡王文汉林李家宓刘旭陆地
Owner KUNMING MEDICAL UNIVERSITY
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