Quinnazolidone derivative, preparation method thereof and purpose of serving as anticarcinogen

Abstract

The invention belongs to the medicine and chemical industry field, which discloses a quinnazolidone derivative, a preparation method thereof and a purpose of serving as anticarcinogen. The structural formula of the quinnazolidone derivative is that: R1 is F, CL, Br or I, R2 is NH (CH2) nNR4, NR4 or NH(CH2)n-Ar, R3 is NHCO (CH2) nNR4 or CONH (CH2) nNR4, and m equals to 1,2 or 3. -Ar represents various aromatic nucleus, including various heteroaromatic compounds; n equals to 1, 2, 3, 4 or 5; R4 represents C1-6alkyl, C3-6 naphthenic base, piperidyl, morpholinyl, piperazine, or quinoxaline and the like or R1 equals to H, R2 equals to R3 equals to NHCO (CH2) nNR4 or R2 equals to H, R1 equals to R3 equals to NHCO (CH2) nNR4, and m equals to 2 or 3. The invention discloses the preparation method of the quinnazolidone derivative and the purpose of serving as the anticarcinogen at the same time. The quinnazolidone derivative has the advantages of strong inhibitory action on the expression of telomere DNA, c-myc and other proto-oncogenes DNA, obvious inhibitory action on various cancer cell strains, little toxicity on normal cells and wide application space on preparing the anticarcinogen.

Description

technical field The invention belongs to the field of medicine and chemical industry, and relates to a quinazolon derivative, a preparation method thereof, and an application thereof in the preparation of anticancer drugs. Background technique Cancer is a major disease that threatens human health and life safety. According to statistics, there are about 4 million new cancer patients in the world every year. The research and development of anticancer drugs has always been a hot spot for chemists and pharmacologists. Finding anticancer drugs with high efficiency, high selectivity and less toxic side effects is one of the important directions of drug research and development. Designing and synthesizing anticancer drugs with DNA as the target, especially designing and synthesizing small molecule inhibitors for the special high-level structure of proto-oncogene DNA such as telomere DNA and c-myc, which have important physiological significance, is the key to the development of n...

AI Technical Summary

Problems solved by technology

Patent application 200810027004 has disclosed a kind of bis-fatty amino substituted quinazolones derivatives and their application as anticancer drugs, however, there are still very few researches on the development of quinazolones at present

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