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Anti-melanoma compound and application thereof

An anti-melanin, compound technology, applied in the field of biomedicine, can solve the problems of high effective dose, no anti-cancer effect of drugs, destruction of the body's immune system, etc., and achieve the effect of inhibiting growth

Inactive Publication Date: 2017-02-01
CHONGQING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chemotherapy is the most common in clinical application, but there are many problems, which mainly focus on the following two aspects: 1. The anti-melanoma drugs currently developed and used in clinic are mainly aimed at patients with gene B-Raf mutation, so if the patient’s B-Raf Without mutations in the Raf gene, the drug has no anticancer effect
2. The effective doses of most clinical drugs are high, causing damage to the body’s immune system, which is not suitable for elderly patients with melanoma
And the patient takes only one drug for a long time, the body is prone to drug resistance, and the effect is not good

Method used

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  • Anti-melanoma compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0011] 1) The compound inhibits the in vitro survival of melanoma cell lines.

[0012] The melanoma cell lines WM858, WM1158 and WM3734 were seeded on 96-well plates at 10,000 cells / 100ul per well. The next day, add the compound with the concentration of 2 and 10 μM and the same volume of DMSO (control group), and use it after 48 hours. The luminescent cell viability assay kit (Promega) was used to quantify the number of viable cells in each treatment group. The method adds a single reagent directly to cultured cells containing serum, eliminating the need for washing cells, removing media, or performing multiple loading steps. The specific steps are: on a 96-well plate, add 20 μl of medium to 100ul The reagents were mixed and detected by a luminescence detector within 10 minutes.

[0013] The results showed that the compound could significantly inhibit the survival of three melanoma cell lines at both high and low concentrations ( figure 1 ), and the inhibition rate was ...

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Abstract

The invention discloses an anti-melanoma compound. The compound is named as N-(3-(5-(2-amino-5-hydroxypyrimidin-4-yl)-2-tert-butylthiazol-4-yl)-2-fluoro-5-hydroxyphenyl)-2,6-difluoro-4-hydroxybenzenesulfonamide, and the structural formula of the compound is represented by formula I. The compound is extracted from a natural product, and is evaluated by using melanoma cell strains and immunodeficiency SCID mouse tumor transplantation models. In vivo and in vitro tests show that the compound can substantially inhibit growth of all melanoma cell strains, and also can effectively inhibit growth of human derived melanoma cells in mouse bodies. The compound has a safe, highly-efficient and ideal anticancer effect, can be processed to possibly develop novel anti-melanoma treatment medicines, and has important development and application values.

Description

technical field [0001] The invention relates to compounds and applications thereof, in particular to an anti-melanoma compound and applications thereof, belonging to the field of biomedicine. Background technique [0002] Melanoma is a malignant tumor of melanocytes mainly in the skin, and it is the skin cancer with the highest mortality rate. It is a rare type of skin cancer, but it has a high degree of malignancy and is one of the leading causes of death from skin cancer. Malignant melanomas vary in size, shape, and color (often hyperpigmented) and in their propensity to invade locally and metastasize distantly. Its clinical manifestations are nodular melanoma, spreading melanoma, lentigo melanoma and special type melanoma. The tumor spreads rapidly and death can occur months after diagnosis. Early, very superficial lesions have a 100% cure rate at 5 years. Therefore, the cure rate depends on early diagnosis and early treatment. [0003] At present, there are not many...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/04A61K31/506A61P35/00
CPCC07D417/04
Inventor 滕勇梁桂兆黄晓斌赵化侃
Owner CHONGQING UNIV
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