Coumarin type derivative and application thereof

A technology of coumarins and derivatives, which is applied in the direction of drug combination, organic chemistry, antineoplastic drugs, etc., can solve problems such as toxic and side effects, and achieve significant antitumor activity and excellent application prospects

Active Publication Date: 2019-01-18
HUAQIAO UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Cytotoxic drugs can kill tumor cells, but they lack selectivity for cancer cells and normal cells, so they have strong toxic and side effects. Looking for targeted anti-tumor drugs that can selectively kill cancer cells and have no effect on normal proliferating cells Drugs have become an important direction for the development of new anticancer drugs

Method used

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  • Coumarin type derivative and application thereof
  • Coumarin type derivative and application thereof
  • Coumarin type derivative and application thereof

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Embodiment Construction

[0028] The present invention relates to a coumarin derivative or a pharmaceutically acceptable salt thereof, the general structural formula of which is shown in I,

[0029]

[0030] Among them, R 1 selected from substituted or unsubstituted aryl or heteroaryl, R 2 Selected from alkyl, substituted or unsubstituted amino, amido, substituted or unsubstituted hydroxyl, carboxyl, ester, C3-C8 heterocyclic group, X is selected from O or S, n is selected from integers from 0 to 6 .

[0031] Preferably, the R 1 is a substituted or unsubstituted phenyl group; the R 2 One selected from hydroxyl group, carboxyl group and substituted amino group; said X is O; said n is selected from an integer of 1-3.

[0032] Preferably, the coumarin derivatives are specifically the following compounds:

[0033] N-[2-(Dimethylamino)ethyl]-7-((2-methyl-[1,1'-biphenyl]-3-yl)methoxy)-2-oxo-2H- benzopyran-3-carboxamide,

[0034] N-[2-(diethylamino)ethyl]-7-((2-methyl-[1,1'-biphenyl]-3-yl)methoxy)-2...

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Abstract

The invention provides a coumarin type derivative or pharmaceutically-acceptable salts thereof. The structural formula of the coumarin type derivative is shown as formula I (which is described in thespecification). The invention also discloses the pharmaceutically-acceptable salts of the coumarin type derivative. The compound provided by the invention has obvious anti-tumor activity and PD-1/PD-L1 inhibiting activity, and can be used for preparing mediciens for treating or preventing cancer diseases and other proliferative diseases, so that the treatment or prevention of the cancer diseases and other proliferative diseases is realized.

Description

【Technical field】 [0001] The invention relates to the technical field of medicine preparation, in particular to a coumarin derivative and its application. 【Background technique】 [0002] Tumor is a disease that seriously threatens human life and health. In recent years, the incidence and mortality of tumors have been increasing year by year. Cytotoxic drugs can kill tumor cells, but they lack selectivity for cancer cells and normal cells, so they have strong toxic and side effects. Looking for targeted anti-tumor drugs that can selectively kill cancer cells and have no effect on normal proliferating cells Drugs have become an important direction for the development of new anticancer drugs. [0003] Immune checkpoints refer to some inhibitory signaling pathways present in the immune system. Under normal circumstances, immune checkpoints can maintain immune tolerance by regulating the intensity of the autoimmune response. However, when the body is invaded by tumors, the acti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/16A61P35/00
CPCA61P35/00C07D311/16
Inventor 马俊杰黄坤倪欣陈柔棻余楚丹闫琦慧陈思颖侯晓林
Owner HUAQIAO UNIVERSITY
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