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Anti-tumor medicament as well as synthetic method and application thereof

A technology of pharmacy and compounds, applied in antitumor drugs, drug combinations, pharmaceutical formulations, etc.

Inactive Publication Date: 2014-11-19
天津天诚新药评价有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, there is no inventive concept of designing drug compounds based on the LATs transporter at home and abroad.

Method used

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  • Anti-tumor medicament as well as synthetic method and application thereof
  • Anti-tumor medicament as well as synthetic method and application thereof
  • Anti-tumor medicament as well as synthetic method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] MS was measured with 4000 QTRAP? LC / MS / MS instrument from AB SCIEX Company, and all were EI sources (70ev) unless otherwise specified; all solvents were redistilled before use, and the anhydrous solvents used were all according to standard The method was obtained by drying; unless otherwise specified, all reactions were carried out at room temperature and followed by TLC. The purification of the product used silica gel (300-400 mesh) column chromatography unless otherwise specified; among them, silica gel (300-400 mesh) Produced by Qingdao Ocean Chemical Factory, GF254 thin-layer silica gel plate is produced by Yantai Jiangyou Silicone Development Co., Ltd.; the prepared product was confirmed by HPLC and MS.

[0048] The preparation of the compound of formula II (doxorubicin-aspartic acid / Doxorubicin-Asp / Asp-DOX), the preparation route is as follows:

[0049]

[0050] The preparation method is prepared by reacting doxorubicin and Fmoc-Asp-OALL with the participation ...

Embodiment 2

[0056] Compound doxorubicin-aspartic acid hydrochloride: Take 1.5 g of the compound purple solid product and dissolve it in 10 mL of absolute ethanol. Cool in an ice-water bath to 5°C, add 11.1% hydrochloric acid ethanol solution dropwise until the pH is 2, and continue to stir for about 1 h in an ice-water bath. Filter and dry in vacuo to obtain a purple solid powder.

Embodiment 3

[0058] Compound doxorubicin-aspartic acid into taurate: Take 2.0 g of the purple solid product of the compound and dissolve it in 10 mL of acetone. After heating to reflux, equimolar taurine was added, and the reaction was stirred for about 1.5 h under reflux. After the reaction was complete, it was left to stand at room temperature for 24 h. Precipitate purple crystals, filter and dry in vacuum to obtain the taurine salt of I.

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Abstract

The invention relates to an anti-tumor medicament namely an amino acid-doxorubicin derivative, a preparation method of the anti-tumor medicament, and an application of the anti-tumor medicament. Specifically, the invention relates to an amino acid-doxorubicin derivative with a structure shown in a formula I, pharmaceutically-acceptable salts of the amino acid-doxorubicin derivative, a medicament composition adopting the compound and the pharmaceutically-acceptable salts of the compound as active and effective components, a preparation method of the amino acid-doxorubicin derivative, the pharmaceutically-acceptable salts and the medicament composition, and an application of the amino acid-doxorubicin derivative, the pharmaceutically-acceptable salts and the medicament composition in treating cancers (liver cancer, acute leukemia, malignant lymphoma, breast cancer, ovarian cancer, soft tissue sarcoma, osteogenic sarcoma, rhabdomyosarcoma, kidney cancer, colon cancer, bladder cancer, thyroid cancer, prostatic cancer, testicular cancer, gastric cancer and the like), and preferentially treating the cancers (liver cancer, colon cancer, breast cancer, prostatic cancer and the like) with over-expressed L-type amino acid transporters (LATs).

Description

technical field [0001] The present invention relates to a targeted drug delivery system of doxorubicin and its structural analogs that can be used to treat cancer, in particular to a system designed in combination with aspartic acid and doxorubicin and its structural analogs A compound, a pharmaceutical composition, a preparation method thereof, and a medical application belong to the field of medicinal chemistry. Background technique [0002] One of the difficult problems in cancer treatment is to target cancer tissue or cancer cells to reduce damage to normal tissues. [0003] The traditional anti-tumor drug doxorubicin and its structural analogues were discovered in the second half of the 19th century and can be widely used to treat various tumors, including leukemia, bladder cancer, breast cancer, gastric cancer, lung cancer, ovarian cancer, thyroid cancer, etc. More effective anticancer drugs for cancer, myeloma, etc. [0004] Although many patent documents have repor...

Claims

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Application Information

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IPC IPC(8): C07H15/252C07H1/00A61K31/704A61P35/00A61P35/02
Inventor 伊秀林武卫党刘昌孝高晶司端运
Owner 天津天诚新药评价有限公司
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