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Application of alkyl indolone derivative and drug resisting thyroid tumor

A technology of alkylindolinone and its derivatives, which is applied in the field of medicine and can solve problems such as poor curative effect and recurrence

Active Publication Date: 2018-07-27
CHINA THREE GORGES UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinically, the treatment methods for papillary thyroid carcinoma are mostly surgical resection and radioactive iodine therapy, but there are problems such as poor curative effect or recurrence after treatment. important treatment for cancer
However, currently effective small molecule drugs for thyroid cancer are urgently needed to be developed

Method used

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  • Application of alkyl indolone derivative and drug resisting thyroid tumor
  • Application of alkyl indolone derivative and drug resisting thyroid tumor
  • Application of alkyl indolone derivative and drug resisting thyroid tumor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] The present invention provides alkylindolinone derivatives, which have the following structure:

[0043]

[0044] where R 1 is ethyl, R 2 is methyl, R 3 For methyl.

[0045] cell culture

[0046] Human Papillary Thyroid Carcinoma BRAF V600EThe mutant cell line BCPAP was cultured with PRMI1640 containing 10% fetal bovine serum, 2mmol / L glutamine, 2mmol / L pyruvine, 2mmol / L non-essential amino acids, 100μg / mL streptomycin sulfate, and 100U / mL penicillin. Cultured in a cell culture incubator at 37°C, 5% CO2 saturated humidity.

[0047] Cell Proliferation Assay

[0048] Inoculate the cells at a density of 2.5×103 / 100 μL and culture them overnight in a 96-well plate. After the cells adhere to the wall, absorb the culture medium in the well plate, and add the alkylindolinone derivatives provided in this example with gradient concentrations. The culture medium continued to culture the cells for 48 h. At the same time, the cells without drug treatment were set as the ...

Embodiment 2

[0064] The alkylindolinone derivative provided in Example 1 is used in combination with the STAT3 inhibitor WP1066, and the drugs with IC30 and IC50 concentrations are combined to measure the inhibition rate, and the CaluSyn software calculates the CI value of the combined drug, CI1 represents synergistic, additive and antagonistic effects respectively, and CI<0.7 represents a strong synergistic effect. It can be seen that the alkylindolinone derivatives provided in Example 1 and WP1066 have a synergistic effect (the following table), and the detection conditions of the inhibition rate With embodiment 1.

[0065]

[0066] The above data show that the combined use of the alkylindolinone derivatives provided in Example 1 and WP1066 has an obvious synergistic effect, and more effective antithyroid tumor drugs can be prepared.

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Abstract

The invention discloses an application of an alkyl indolone derivative and a drug resisting thyroid cancer. The alkyl indolone derivative has a remarkable cancer cell inhibition effect when applied topreparation of anti-cancer drugs. The drug resisting thyroid cancer contains the alkyl indolone derivative with concentration being 0.025 mu M or higher and has remarkable thyroid cancer resistant effect.

Description

technical field [0001] The invention belongs to the field of medicine, and more specifically relates to the application of an alkylindolinone derivative and an antithyroid tumor drug. Background technique [0002] The etiology of malignant cancer is not fully understood. Years of epidemiological research and experimental and clinical observations have found that environment and behavior have an important impact on the occurrence of human malignant cancer. It is estimated that more than 80% of malignant cancers are related to environmental factors. Various environmental and genetic carcinogenic factors may cause non-lethal DNA damage in a synergistic or sequential manner, thereby activating proto-oncogenes or / and inactivating cancer suppressor genes, plus apoptosis-regulating genes and ( or) Alterations in DNA repair genes that transform cells. Transformed cells can first exhibit polyclonal proliferation, and go through a long multi-stage evolution process, in which a cert...

Claims

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Application Information

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IPC IPC(8): A61K31/404C07D209/34A61P35/00
CPCA61K31/404C07D209/34
Inventor 邓鹏裔崔邦平卢乔苗代文莉王朋田金玲高雯琪
Owner CHINA THREE GORGES UNIV
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