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Antineoplastic medicament antifolate, its salt and midbody

An anti-folate agent and anti-tumor technology, which is applied in the field of anti-tumor drug anti-folate agent and its salts and intermediates, and compounds, can solve the problems of solid tumors with little effect, unsatisfactory treatment effect, and strong disease, and achieve Strong growth inhibitory activity, the effect of overcoming the problem of drug resistance

Inactive Publication Date: 2008-06-11
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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  • Antineoplastic medicament antifolate, its salt and midbody
  • Antineoplastic medicament antifolate, its salt and midbody
  • Antineoplastic medicament antifolate, its salt and midbody

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Embodiment Construction

[0030] The embodiments of the present invention are described in detail below: the present embodiment is implemented under the premise of the technical solution of the present invention, and detailed implementation and specific operation process are provided, but the protection scope of the present invention is not limited to the following implementation example.

[0031] This type of antifolate of the present invention and salt thereof can be synthesized by various methods, hereinafter referred to as R 1 =NH 2 and R 2 =CH 3 , or R 1 =NHCH 3 and R 2 =H, Ar is 1,4-phenyl or 2,5-thienyl as an example to illustrate the synthesis route of the present invention, but not limited to this functional group.

[0032] step 1

[0033] Synthesis of 4-[3-(2,4-diamino-6-methylamino-pyrimidin-5-yl)-4-nitro-butyl]-benzoic acid methyl ester 1

[0034] Reaction formula:

[0035]

[0036] 4-(4-Nitro-but-3-enyl)-benzoic acid methyl ester (0.69g, 2.93mmol) and 2,4-diamino-6-(methylamino...

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PUM

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Abstract

The invention discloses an antifolic for anti-tumor therapy, a relative salt and intermediate, wherein the antifolic and relative salt are represented as below, R1=NH2, R2=CH3, or R1=NHCH3 and R2=H, Ar is 1, 4-phenyl or 2, 5-thiofuran, R3 is H, metal cation, ammonium ion, or organic ammonium cation. The invention further discloses an application of the antifolic and relative salt for preparing anti-cancer drug. The inventive antifolic and relative salt have significant growth restraining activity on multiple tumor cells.

Description

technical field [0001] The invention relates to a compound in the technical field of medicine and chemical industry, in particular to an antifolate agent used for antitumor drugs and its salt and intermediate. 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 drugs. [0...

Claims

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Application Information

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IPC IPC(8): C07D487/04A61K31/519A61P35/00
Inventor 毛振民刘增路朱高军
Owner SHANGHAI JIAO TONG UNIV
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