Artemisinin-chlorambucil ester compound and preparation method thereof

A technology of chlorambucil and chlorambucil, which is applied in the field of artemisinin-chlorambucil synthesis and its preparation, can solve the problems of severe toxic and side effects, achieve low toxic and side effects, reduce Toxic and side effects, strong anti-tumor activity
CN112920198APending Publication Date: 2021-06-08江苏德信辰科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
江苏德信辰科技有限公司
Publication Date
2021-06-08

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Abstract

The invention belongs to the technical field of artemisinin derivatives, and particularly relates to an artemisinin-chlorambucil ester compound and a preparation method thereof. In order to solve the problems that the tumor effect of artemisinin needs to be improved, the toxic and side effects of chlorambucil are large and the like, artemisinin-chlorambucil ester with a novel structure is designed and synthesized according to a pharmacophore splicing principle, and the structure of the artemisinin-chlorambucil ester compound is represented and determined by 1H NMR, 13C NMR and HRMS-ESI. The compound has good anti-tumor activity, and the toxic and side effects of chlorambucil are reduced. The preparation method is simple, the obtained derivative is high in anti-tumor activity and low in toxic and side effects, a novel medicine is provided for tumor resistance, and the derivative has good application value.
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Description

technical field

[0001] The invention belongs to the technical field of artemisinin derivatives, in particular to an artemisinin-chlorambucil compound and a preparation method thereof. Background technique

[0002] Artemisinin is a natural product of sesquiterpene lactones isolated from Artemisia annua of Compositae, and its structure contains a unique peroxy bridge structure. Studies have shown that artemisinin has a variety of important pharmacological activities, such as insect resistance, anti-tumor and anti-inflammation. Due to the poor pharmacokinetic properties of artemisinin, people have done a lot of derivation and modification of its structure, and a variety of artemisinin derivatives are used in clinical antimalarial treatment, such as artemether, artesunate, etc. Drugs can effectively reduce the mortality rate of malaria patients and save the lives of tens of thousands of patients. Chinese scientist Tu Youyou won the 2015 Nobel Prize in Physiology or Medicine fo...

Claims

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