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Theanine and RGDS co-modified 5-fluorouracil as well as synthesis, activity and application thereof

A fluorouracil and reaction technology, which can be used in medical preparations containing active ingredients, drug combinations, peptide/protein components, etc., and can solve problems such as failure to achieve expected effects.

Active Publication Date: 2021-02-23
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But it didn't work as expected

Method used

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  • Theanine and RGDS co-modified 5-fluorouracil as well as synthesis, activity and application thereof
  • Theanine and RGDS co-modified 5-fluorouracil as well as synthesis, activity and application thereof
  • Theanine and RGDS co-modified 5-fluorouracil as well as synthesis, activity and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1 prepares Boc-Arg (NO 2 )-Gly-OBzl

[0020] 3.19g (10mmol) Boc-R(NO 2 ) was dissolved in anhydrous tetrahydrofuran (THF), and 1.35 g (10 mmol) of 1-hydroxybenzotriazole and 2.68 g (13 mmol) of dicyclohexylcarbodiimide were sequentially added to the resulting solution. After stirring for 30 min, 3.71 g (1.1 mmol) of Gly-OBzl in tetrahydrofuran was added to the reaction solution, and N-methylmorpholine was added dropwise to the reaction solution at 0°C to adjust the pH to 8. The reaction solution was stirred at room temperature until TLC showed that the reaction was complete. The reaction mixture was filtered, the filtrate was concentrated under reduced pressure, and the residue was dissolved in ethyl acetate solution. Purification by silica gel column chromatography gave 3.53 g (75%) of the title compound as a colorless solid. ESI-MS(m / e): 467[M+H] + .

Embodiment 2

[0021] Example 2 Preparation of Boc-Asp(OBzl)-Ser-OBzl

[0022] Using the method of Example 1, 3.86g (77%) of the title compound was obtained as a colorless solid from 3.32g (10mmol) Boc-Asp(OBzl) and 2.78g (1.2mmol) Ser-OBzl. ESI-MS(m / e): 501[M+H] + .

Embodiment 3

[0023] Embodiment 3 prepares Boc-Arg (NO 2 )-Gly

[0024] 5.33g (5mmol) Boc-Arg(NO 2 )-Gly-OBzl was dissolved in methanol, and the pH value of the reaction solution was adjusted to 13 with sodium hydroxide solution (2M). Continue the reaction at 0°C until the reaction is complete as monitored by TLC. The pH of the reaction was adjusted to neutral with 2N hydrochloric acid solution. Concentrate under reduced pressure to remove methanol. Continue to add 2N hydrochloric acid solution dropwise at 0°C to adjust the pH value to 2. The solution was extracted with ethyl acetate. The ethyl acetate layer was washed with saturated aqueous sodium chloride until neutral, and dried by adding anhydrous sodium sulfate. After filtration, the filtrate was concentrated under reduced pressure to remove the solvent to obtain 1.63 g (86%) of the title compound as a white solid. ESI-MS(m / e): 375[M-H] - .

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Abstract

The invention discloses theanine and RGDS co-modified 5-fluorouracil in the following formula. The invention also discloses a preparation method and anti-tumor and anti-tumor metastasis activity of 5-fluorouracil. Therefore, the invention discloses an application of 5-fluorouracil in preparation of anti-tumor drugs, an application of 5-fluorouracil in preparation of anti-tumor metastasis drugs andan application of 5-fluorouracil in preparation of drugs with anti-tumor and anti-tumor metastasis dual activities.

Description

technical field [0001] The present invention relates to compound 1-(CH 2 CO-The)-3-(CH 2 (CO-Arg-Gly-Asp-Ser)-5-fluorouracil, relates to its preparation method, relates to its anti-tumor activity and anti-tumor metastasis activity, thus the present invention relates to its application in the preparation of anti-tumor drugs, relates to its use in The application in the preparation of anti-tumor metastasis drugs, and its application in the preparation of anti-tumor and anti-tumor transfer drugs. The invention belongs to the field of biomedicine. Background technique [0002] 5-Fluorouracil (5-FU) is a pyrimidine antimetabolite antineoplastic drug with a broad antitumor spectrum. It is mostly used in the treatment of digestive tract tumors, breast cancer, ovarian cancer, bladder cancer, and liver cancer. 5-FU has some defects in clinical application. For example, the oral first-pass effect is obvious, and the clinical route of administration is intravenous injection. The ...

Claims

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Application Information

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IPC IPC(8): C07K7/06A61K38/08A61P35/00A61P35/04
CPCC07K7/06A61P35/00A61P35/04A61K38/00Y02P20/55
Inventor 赵明彭师奇康贵峰任智奇
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES