Guanidyl-containing artemisinin derivates and application thereof

Abstract

The invention relates to artemisinin derivates as shown in a general formula I, optically active isomers and pharmaceutically acceptable salts thereof, wherein the substituents R1, R2, X and Ar have the meanings defined in the specification. The invention also relates to application of the compound shown in general formula I in the preparation of medicaments for treating and / or preventing cancer.

Description

technical field The invention belongs to the technical field of medicine, and relates to new artemisinin derivatives and their optically active bodies, and their pharmaceutically acceptable salts, their preparation methods and pharmaceutical compositions containing the compounds. The present invention also relates to the use of the derivative in the preparation of medicines for treating and / or preventing cancer and other proliferative diseases. Background technique Cancer is a disease that seriously threatens human life. According to the statistics of WHO in 2008, the number of cancer deaths in 2007 reached 7.9 million, accounting for about 13% of all deaths. In recent years, with the deepening of the research on the mechanism of tumorigenesis, the molecular mechanism of the occurrence and development of cancer has been continuously revealed, and anti-tumor drugs have developed from the initial cytotoxic drugs to the research on drugs that act on tumor-specific targets. Ar...

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Problems solved by technology

When studying the anticancer activity of artesunate on 55 cancer cell lines, Eferth et al. found that artesunate had the strongest anticancer activity on leukemia cells and colon cancer cells, and had the strongest anticancer activity on melanoma, breast cancer, ovarian cancer, Prostate cancer, central nervous system tumors and kidney cancer cells have moderate activity, and the activity to non-small cell lung cancer cells is the weakest

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