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Repurposed antibiotics for non-nuclear genotoxic chemotherapy and pharmaceutical composition for Anti-cancer containing the same

A technology of compounds and antibiotics, applied in drug combinations, chemical instruments and methods, active ingredients of phosphorus compounds, etc., to achieve the effect of preventing cancer recurrence

Pending Publication Date: 2021-12-28
诊疗化学公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, antibiotics have no effect on the large number of cancer cells that make up 99% of the total cancer volume, and they inhibit the division and growth of cancer stem cells instead of killing them
That is, these studies only indicate a possible therapeutic effect of antibiotics

Method used

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  • Repurposed antibiotics for non-nuclear genotoxic chemotherapy and pharmaceutical composition for Anti-cancer containing the same
  • Repurposed antibiotics for non-nuclear genotoxic chemotherapy and pharmaceutical composition for Anti-cancer containing the same
  • Repurposed antibiotics for non-nuclear genotoxic chemotherapy and pharmaceutical composition for Anti-cancer containing the same

Examples

Experimental program
Comparison scheme
Effect test

Synthetic example 1

[0057] Synthesis Example 1: Synthesis of Ester Mt-CFX

[0058] Ester Mt-CFX was synthesized according to Scheme 1:

[0059] [Option One]

[0060]

[0061] Compounds 1 and 2 shown in Scheme 1 were synthesized according to methods known in the art.

[0062] (1) Synthesis of compound 3

[0063] Compound 1 (1 g, 1.975 mmol) and Compound 2 (852 mg, 1.975 mmol) were dissolved in dimethylformamide as a solvent, and then potassium carbonate (819 mg, 5.925 mmol) was slowly added thereto. The mixture was stirred at 50°C for 12 hours. The reaction mixture was evaporated under reduced pressure to remove solvent. The residue was purified by column chromatography and dissolved in 50 mL of a mixed solution of methanol and distilled water (1 / 9). Add NaBF to the solution 4 , followed by stirring for 1 hour. The reaction mixture was extracted with dichloromethane and distilled water and dissolved in methanol. adding After 1 x 8 chloride, the resulting mixture was stirred for 6 ho...

Synthetic example 2

[0067] Synthesis Example 2: Synthesis of Amide Mt-CFX

[0068] The amide Mt-CFX was synthesized according to Scheme 2:

[0069] [Option II]

[0070]

[0071] Compounds 1 and 2 shown in Scheme 2 were synthesized according to methods known in the art.

[0072] (1) Synthesis of Compound 4

[0073] Compound 1 (1 g, mmol) was dissolved in 35 mL of 7N NH in methanol 3in solution. The solution was stirred at room temperature for 3 days. Thereafter, the reaction solution was evaporated under reduced pressure to remove the solvent. The residue was purified by column chromatography.

[0074] (2) Synthesis of compound 5

[0075] Compound 2 (1 g, 2.318 mmol), EDC hydrochloride (667 mg, 3.477 mmol) and 1-hydroxybenzotriazole hydrate (470 mg, 3.477 mmol) were dissolved in dimethylformamide as a solvent. The solution was stirred at room temperature for 30 minutes. To the reaction solution were added DMAP (425 mg, 3.477 mmol) and compound 4 (1.025 g, 2.318 mmol). The resulting ...

experiment example

[0080] 1-1. Animal cell culture

[0081] Human metastatic breast cancer cell line MDA-MB-231 (human breast cancer cells), lung cancer cell line A549 (human lung cancer cells), human colon cancer cell line SW620 (human colon cancer cells), human prostate cancer cell line DU145 and PC3 (human prostate cancer cells) were cultured in RPMI1640 medium and modified Eagle's medium (modified Eagle's media, MEM). All media were supplemented with 10% inactivated fetal bovine serum (FBS) and 1% penicillin-streptomycin. All cell lines were cultured at 37°C and 5% carbon dioxide.

[0082] 1-2. Cell viability analysis

[0083] MDA-MB-231, A549, SW620, DU145 and PC3 cells were seeded into 96-well plates and cultured overnight for stabilization. After the stabilized cells were treated with different concentrations of ester MT-CFX, amide MT-CFX and ciprofloxacin from 0 to 100 μM for 48 hours, the amount of LDH in living cells was measured to determine cell viability. Data are shown as m...

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Abstract

The present invention relates to a repurposed antibiotic compound for the treatment of cancer with minimal nuclear gene damage and an anticancer pharmaceutical composition comprising same. Since the repurposed antibiotic compound has a therapeutic effect in a manner that targets only the mitochondria of cancer cells, the modified antibiotic compound does not cause gene degeneration unlike conventional chemotherapy which damages nuclear DNAs to kill cancer cells,, thereby preventing the recurrence of cancer. In addition, a mitochondria targeted therapy using the compound according to the present invention can effectively treat malignant tumors that are difficult to treat due to acquiring drug resistance by general anticancer treatment.

Description

technical field [0001] The present invention relates to modified antibiotic compounds for cancer treatment with minimal damage to nuclear genes and anticancer pharmaceutical compositions comprising said compounds. Background technique [0002] Many research groups around the world have devoted themselves to the development of different drug delivery systems to enhance the therapeutic effect of existing anticancer drugs with reduced side effects, and as a result, have successfully developed the effective A drug delivery system that delivers to cancer tissues and enables anticancer drugs to be activated only in the cancer microenvironment achieves significantly improved cancer treatment safety. [0003] However, despite these technological advances, the treatment and suppression of recurrent and metastatic cancers with acquired drug resistance remains a challenge for conventional anticancer therapies. 90% of cancer deaths are caused by recurrent cancers rather than primary ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6558A61K31/675A61P35/00
CPCC07F9/65583A61P35/00A61K47/54A61K31/66A61K31/496C07F9/6561
Inventor 金钟昇鲜于卿彼得·维威尔斯特元美爱
Owner 诊疗化学公司
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