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Methylamino-pterin derivative with inhibiting nitric oxide synthetase function

A compound, methyl technology, applied in the field of methotrexate derivatives, can solve problems such as expanding the anti-cancer spectrum, protein synthesis obstacles, and severe toxicity

Inactive Publication Date: 2005-02-23
CHINA PHARM UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

④ NO is toxic to DNA and hinders protein synthesis
[0027] For half a century, MTX has been a clinically important anti-cancer drug, immunosuppressant and anti-rheumatic arthritis drug, etc., but because of its narrow anti-cancer spectrum, it is also a non-selective cytotoxic agent. Greater toxicity; moreover, MTX has been used clinically for more than 50 years, and the drug resistance of cancer cells to MTX has been revealed. Therefore, since MTX has been used clinically, many medicinal chemists abroad have been modifying its structure , to reduce its toxicity and expand its anticancer spectrum

Method used

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  • Methylamino-pterin derivative with inhibiting nitric oxide synthetase function
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  • Methylamino-pterin derivative with inhibiting nitric oxide synthetase function

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Experimental program
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Embodiment Construction

[0076] 1. Instruments and reagents:

[0077] The melting point of each compound in this experiment was determined by Mel-TEMP melting point apparatus, and the temperature was not corrected. MS was determined by HP1100LC / MSD mass spectrometer. Silica gel GF for thin layer chromatography (TLC) plates 254 (Qingdao Ocean Chemical Factory) and 0.8% CMC-Na distilled aqueous solution are stirred evenly and then paved, then activated at 100-110°C for 1h, placed in a desiccator for future use, and placed under an ultraviolet lamp (wavelength 254nm and 365nm) for color development; column chromatography adopts 100-200 or 200-300 mesh silica gel (produced by Qingdao Ocean Chemical Factory), and the column is packed by dry method. The H-NMR spectrum is measured with a BruckAV-300 nuclear magnetic resonance instrument, without special instructions, the solvent used is D 6 -DMSO. Elemental analysis was determined with an Elementar Vario ELIII instrument. Reagents are commercially avail...

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Abstract

This invention relates to methylaminopterin derivatives with 4-amino structure modified, which inhibit effect of nitrogen monoxide synthetase and growth of tumors. They have wide anti-cancer spectrum and little toxic side effect so as to be used in preparation of medicines for tumors, cancers, arthritis and intestinal diseases as well as chemicals for birth control.

Description

technical field [0001] The present invention relates to a new class of MTX derivatives, and specifically relates to a methotrexate derivative with the effect of inhibiting nitric oxide synthase, which can improve the anti-tumor and anti-articular effects of the clinical drug MTX (methotrexate) Inflammation, treatment of intestinal diseases, as the activity of family planning, etc. Background technique [0002] (1) Biochemical and pharmacological effects of MTX and its application [0003] Tetrahydrofolates (abbreviated as THF) derivatives are extremely important substrates for various enzymes of one-carbon metabolism in cells, that is, donors of formyl, hydroxymethyl or methyl in pyrimidine and purine biosynthesis , plays an important role in the processes of DNA and RNA synthesis, replication and repair. The synthesis of tetrahydrofolate in cells is completed by folic acid through the action of dihydrofolate reductase (Dihydrofolate reductase, DHFR). Folic acid and metho...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61P1/16A61P3/10A61P7/00A61P9/02A61P9/10A61P25/00A61P31/12C07D475/08
Inventor 姚其正冯明声石静波姜力勋郭平
Owner CHINA PHARM UNIV
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