Derivative of folacin alkylation and application

Abstract

This invention provides a folic acid alkylated derivatives, more specifically, folic acid stearyl amine derivative I and folic acid stearic acid derivative II, which are obtained by coupling reaction of folic acid amino and stearic acid carboxyl, or folic acid carboxyl and stearyl amine amino. The folic acid alkylated derivatives can be used to prepare folic acid modified lipid nanoparticles. The alkyl chains of the derivatives have compatibility with lipid nanoparticles, which can accelerate the absorption of lipid nanoparticles, and increase the tumor targeting performance of lipid nanoparticles. The folic acid alkylated derivatives can be used in preparing folic acid modified lipid nanoparticles carrying antitumor drugs. The structural formula of the folic acid alkylated derivatives is shown in this invention.

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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