Naphthopyrone compounds, and preparation method and application thereof

Abstract

The invention relates to naphthopyrone compounds, and a preparation method and application thereof, belonging to the field of pharmaceutical chemistry. The six naphthopyrone compounds have the advantages of simple preparation process, simple raw materials, convenient after-treatment, high yield and high purity (up to 98% or above), and the structure can be verified through nuclear magnetism and mass spectroscopy. After the six naphthopyrone compounds are used for preparing antineoplastic drugs and the obtained antineoplastic drugs are subjected to anticancer activity research on A549 cells (human non-small cell lung cancer cells), the research result on the apoptosis by the real-time cell analysis technique (RTCA) proves that the compounds L2 and L3 have strong killing actions on the A549 cells, the compound L1 has weaker killing actions, and the compounds L4, L5 and L5 have the weakest killing actions. Therefore, the invention has substantial meanings for research into screening of the antineoplastic drugs of the compounds.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a naphthopyrone compound with biologically active small organic molecules and a preparation method and application thereof. Background technique [0002] Coumarins, also known as benzo-α-pyrones (formula 1 below), are an important class of oxygen-containing heterocyclic compounds, which play a pivotal role in natural product compounds. Most of the coumarin compounds that have been discovered have oxygen-substituted functional groups at the C-7 position, so 7-hydroxycoumarin (umbelliferone, the following formula 2) is considered to be the parent of coumarin compounds. With the advancement of modern synthesis, extraction, separation, and analysis methods, more coumarin compounds with higher pharmacological activity have been discovered one after another, and are effectively used in the process of fighting human diseases. [0003] [0004] Coumarin compounds were f...

AI Technical Summary

Problems solved by technology

[0010] Although people have conducted extensive research on the pharmacological activity of coumarins and tried to develop them into clinical drugs, so far, there are very few varieties that have become clinical drugs.

In particular, coumarin-based drugs for the treatment of tumors have not been reported

A large number of coumarins have limited sources and are unstable, especially the lactone ring structure; and some structures have poor solubility and poor targeting for certain diseases

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