Two nitrogen mustard derivatives, as well as preparation method and application therefore in tumor treatment

Abstract

The invention discloses novel nitrogen mustard derivatives. The nitrogen mustard derivatives are characterized in that a nitrogen mustard alkylation group is at one end, a 6,7-substituted quinazoline structure is at the other end, the substituent R1 is located at the 4th position of the quinazoline main body and is 2-nitrogen mustard group or 3-nitrogen mustard group, morpholinepropoxy and methoxy are located at the 6th position and the 7th position of the quinazoline main body, and the structural formula is shown in formula A. Experiments prove that the compounds can inhibit the cell cycle at the G2 / M period and are di-functional alkylation agents. The in-vivo anti-tumor activity experiments prove that the compounds are quite good in activity. In addition, the compounds have the superiority to other nitrogen mustard medicines, namely, the compounds are quite low in toxicity. Simultaneously, the compounds are easy to synthesize, and quite high in total yield. All the above advantages prove that the compounds have great potential to function as medicines for treating tumors.

Description

Technical field: [0001] The invention relates to two novel nitrogen mustard derivatives, their preparation method and their application as tumor treatment drugs. Background technique: [0002] Tumor is a disease that seriously threatens human health. Over the years, scientists from various countries have made unremitting efforts to find out more suitable tumor chemotherapy drugs for tumor treatment. [0003] Nitrogen mustards are the earliest anti-tumor alkylating agents used clinically. Since their inception, the development of new nitrogen mustards has been going on for a long time. In the development process of nitrogen mustard drugs, how to introduce new drug carriers to reduce drug toxicity and increase tumor selectivity, thereby improving the therapeutic index, is the common goal of scientists from all over the world. At present, research based on this idea is mainly focused on the following three directions: introducing sugars and their derivatives into drug molecul...

AI Technical Summary

Problems solved by technology

So far, there are only a few reports on the research of nitrogen mustard compounds with quinazoline derivatives as anti-tumor drugs, and the potential of these compounds as anti-tumor drugs has not been fully tapped.

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