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Folid acid derivatives and their salts for preparing antitumor medicine

A technology of folic acid derivatives and drugs, applied in the fields of chemistry and medicine, can solve the problems of solid tumors with little effect, unsatisfactory treatment effect, toxicity, etc., and achieve the effect of overcoming drug resistance and strong growth inhibitory activity

Inactive Publication Date: 2008-12-10
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] MTX mainly fights cancer through folic acid antagonism, has strong toxicity, and has little effect on solid tumors. There is also resistance of tumor cells to this drug, so satisfactory therapeutic effects cannot be obtained.

Method used

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  • Folid acid derivatives and their salts for preparing antitumor medicine
  • Folid acid derivatives and their salts for preparing antitumor medicine
  • Folid acid derivatives and their salts for preparing antitumor medicine

Examples

Experimental program
Comparison scheme
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Embodiment Construction

[0031] This type of folic acid derivatives and salts thereof of the present invention can be synthesized by various methods, hereinafter referred to as R 1 =NH 2 , R 2 =CH 3 and CH 2 CH 3 As an example, to illustrate the synthetic route of the present invention, but not limited to this functional group.

[0032] step 1

[0033] Synthesis of 2,4-diamino-5-cyano-7hydro-pyrrolo[2,3-d]pyrimidine (1)

[0034] Reaction formula:

[0035]

[0036] Sodium acetate (13.1 g, 96 mmol) was added to 180 ml of distilled water, and then 2,4,6-triaminopyrimidine (6.0 g, 48 mmol) was added, heated to 50° C., and the solid dissolved. Maintaining the temperature at 50°C, 2-chloro-3-oxo-propionitrile solution (40ml) was slowly added dropwise over 1.5h. The solution turned from colorless to orange-red and then gray-brown. Stirring and reaction were continued at this temperature for 12 hours, the remaining THF in the solution was distilled off under reduced pressure, and then the temperatur...

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PUM

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Abstract

The present invention discloses a kind of folic acid derivatives and their salts for preparing antitumor medicine. The present invention discloses the application of these folic acid derivatives and their salts in preparing medicine for treating cancers. These folic acid derivatives and their salts have powerful tumor cell growth inhibiting activity.

Description

technical field [0001] The invention relates to a class of folic acid derivatives and salts thereof, which can be used to prepare medicines for treating cancer, and belong to the technical fields of chemistry and medicine. Background technique [0002] Reduced folic acid (FH 4 ) is an essential one-carbon unit transporter in the biosynthesis of purines and the conversion of deoxyuridine monophosphate (dUMP) to thymidylate (dTMP). In these biochemical reactions, reduced folic acid is oxidized and regenerated into active reduced folic acid by dihydrofolate reductase (DHFR). [0003] Methotrexate (MTX) and similar compounds are known to bind strongly to DHFR, and these drugs inhibit the reduction of dihydrofolate to tetrahydrofolate, resulting in dTMP and / or purine deficiency, disruption of DNA synthesis, and subsequent cytotoxicity effect, leading to cell death. These drugs have been developed into anticancer drugs, and currently occupy a very important position as clinical...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04A61K31/519A61P35/00C07D239/00C07D207/00
Inventor 毛振民刘增路朱高军
Owner SHANGHAI JIAO TONG UNIV
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