Derivative of folacin alkylation and application

Abstract

The invention provides a folic acid alkylated derivative, specifically stearylamine derivative I of folic acid and stearic acid derivative II of folic acid, which consist of the amino group of folic acid and the carboxyl group of stearic acid, or the carboxyl group of folic acid and stearic acid The coupling reaction of the amino group of the amine is synthesized. The folic acid alkylated derivatives provided by the present invention can prepare folic acid-modified lipid nanoparticles, so as to achieve the purpose of folic acid modification of lipid nanoparticles, through the affinity of the alkyl chain in the derivative and the lipid material, and Through the folic acid receptor-mediated pathway overexpressed on the surface of tumor cells, the cellular uptake of lipid nanoparticles is accelerated, thereby improving the anti-tumor targeting of the lipid nanoparticle anti-tumor drug delivery system, which can be used in the preparation of folic acid-modified loaded anti-tumor Applications of drug solid lipids and nanostructured lipid carriers in drug delivery systems. The structural formula of the compound of the present invention is.

Description

technical field [0001] The invention belongs to a synthesis method of compounds, and relates to the synthesis of folic acid alkylated derivatives and their application in antitumor therapy. Background technique [0002] Tumor has always been a major disease that directly threatens human health. Due to the lack of molecular targeting of the drug itself, tumor chemotherapy has major treatment problems such as low cure rate and huge toxic side effects. Directly targeting drugs to diseased tissues (organs) and cells through appropriate carrier technology is one of the important means to solve the low cure rate and toxic side effects of cancer chemotherapy. At present, scientists at home and abroad have made some progress in the tissue (organ) and cell targeting of tumor drugs through carrier technology, but have not achieved breakthrough curative effects. The essence is that the molecular targets of most anti-tumor drugs are located in Intracellular, so the research and develop...

AI Technical Summary

Problems solved by technology

However, the simple physical encapsulation of folic acid with such carriers will, on the one hand, cause a large amount of folic acid leakage during the in vivo transport process, and on the other hand, it may be encapsulated in or distributed in lipid materials. Thus affecting the tumor cell targeting effect of folic acid

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