Garcinia derivative, method for preparing same and pharmaceutical application thereof

Abstract

The invention relates to the field of pharmaceutical chemistry, in particular to a garcinia derivative(I), a method for preparing the same and pharmaceutical application thereof. The definitions of R1 and R2 are specified in the description. The derivative of the invention is a structure-simplified analogue of gambogic acid compounds, has the anti-tumor effect and can be used for preparing anti-tumor medicaments.

Description

technical field The invention relates to the field of medicinal chemistry, in particular to a class of Garcinia derivatives, a preparation method thereof and an application in pharmacy. The derivative is a structure simplification of gambogic acid compound, has antitumor effect and can be used for preparing antitumor drugs. Background technique The natural product, gambogic acid, was first extracted from the garcinia resin of the genus Garcinia, and it is an important anti-tumor active ingredient in the garcinia resin. Studies have shown that gambogic acid can selectively kill various tumor cells without affecting the normal hematopoietic system and immune function. Gambogic acid can also bind to a variety of proteins related to tumorigenesis and invasion to induce apoptosis, and can be used as an effective apoptosis inducer for various tumor lines. The structural formula of gambogic acid is as follows: Due to the large molecular weight of gambogic acid, adding correspon...

AI Technical Summary

Problems solved by technology

Due to the large molecular weight of gambogic acid, adding corresponding groups in the structural modification may lead to unsatisfactory druggability, and the source of gambogic acid depends on the extraction and separation of natural products, which is not conducive to industrial production

There are relevant literatures reporting that its structure simplifies II, and through anti-pharmacological tests, it is found that the anti-tumor activity is much lower than that of gambogic acid, and it does not have the characteristics of druggability