Tricyclic furo[2, 3-d]pyrimidone compounds and application thereof

Abstract

The invention relates to compounds. Cyanoethyl acetate and chloroacetone with different substituent groups are used as initial raw materials, a cyanoethyl ester compound is generated under the action of sodium ethoxide, then furan compounds are generated through intramolecular ring closing under the action of trifluoroacetic acid, the furan compounds respectively react with 2-pyrrolidone, valerolactam and caprolactam under the action of phosphorus oxychloride to form a ring, so as to obtain furo[2, 3-d]pyrimidinone compounds, and then oxygen-sulfur exchange is performed under the action of phosphorus pentasulfide, so as to obtain the furo[2, 3-d]pyrimidinethione compounds. The 54 kinds of obtained tricyclic furo[2, 3-d]pyrimidone compounds are used as positive control of DOX, the inhibitory activity of Hela cervical cancer cells, MCF-7 breast cancer cells and A549 lung cancer cells is achieved, and results show that the compounds C11 and C17 have the inhibitory activity of the Hela cervical cancer cells; the compounds D5 and D7 have inhibitory activity on A549 lung cancer cells; and the compound C14 has inhibitory activity on MCF-7 breast cancer cells.

Description

technical field

[0001] The invention relates to a tricyclic furo[2,3-d]pyrimidinone compound and its use. The results of cell activity screening of the compound show that two compounds have inhibitory activity on Hela cervical cancer cells; one compound It has inhibitory activity on MCF-7 breast cancer cells; 2 compounds have inhibitory activity on A549 lung cancer cells. Background technique

[0002] According to the statistics of the World Health Organization (WHO), there are about 10 million cancer cases worldwide each year, and about 7 million deaths. In my country, the annual cancer incidence is about 1.2 million, and the number of cancer deaths is as high as 900,000 or more. [1,2] , has become the second killer of human after cardiovascular disease. Although most of the chemically synthesized anticancer drugs also produce toxic and side effects on normal cells of the human body. However, there are few reports on finding anticancer active ingredients with low toxicity...

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