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Semicarbazone derivative serving as caspase-3 activator and application thereof

A technology of semicarbazides and derivatives, applied in the fields of drug combination, organic chemistry, anti-tumor drugs, etc., can solve problems such as inability to deliver correctly, and the inability of anti-tumor drugs to inhibit tumor cell growth.

Inactive Publication Date: 2019-01-25
HUAQIAO UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

What's more worth mentioning is that procaspase-3 belongs to the downstream protein in the apoptosis signaling pathway. If the occurrence of cancer is caused by the mutation of the downstream protein, the upstream apoptosis signal will not be correctly transmitted to the downstream protein, resulting in the effect of Antineoplastic drugs targeting mid / upstream apoptotic signals will not be able to inhibit tumor cell growth

Method used

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  • Semicarbazone derivative serving as caspase-3 activator and application thereof
  • Semicarbazone derivative serving as caspase-3 activator and application thereof
  • Semicarbazone derivative serving as caspase-3 activator and application thereof

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Experimental program
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Embodiment Construction

[0041] The invention relates to a semicarbazone derivative or a pharmaceutically acceptable salt thereof used as a caspase-3 activator, characterized in that: its general structural formula is as shown in I,

[0042] ;

[0043] in,

[0044] K is O, S;

[0045] M is a C6-C10 aryl group, or a 5-10 membered heteroaryl group, and the heteroaryl group contains 1-3 heteroatoms selected from O, N and S;

[0046] R 1 and R 2 The same or different, independently selected from hydrogen, (C 1 -C 10 ) Alkyl, (C 3 -C 7 ) cycloalkyl, (C 2 -C 10 ) alkenyl or (C 2 -C 10 ) alkynyl;

[0047] or R 1 and R 2 Together with the nitrogen atoms they are connected to form a 4-10 membered heterocyclic group, the heterocyclic group except with R 1 and R 2 In addition to the connected nitrogen atom, it optionally contains 1-4 heteroatoms selected from N, O and S;

[0048] R 3 is hydrogen, (C 1 -C 10 ) Alkyl, (C 3 -C 7 ) cycloalkyl, (C 2 -C 10 ) alkenyl, (C 2 -C 10 ) alkynyl, a...

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Abstract

The invention provides semicarbazone derivative serving as a caspase-3 activator and application thereof. A structural general formula of the semicarbazone derivative or pharmaceutically acceptable salts of the semicarbazone derivative is shown as a formula I shown in the description. The semicarbazone derivative disclosed by the invention can be applied to preparing of medicine for treating or preventing cancer diseases and other hyperplastic diseases; thus, treating or preventing the cancer diseases and other hyperplastic diseases, and the semicarbazone derivative has an excellent application prospect in the aspect of developing antineoplastic medicine.

Description

【Technical field】 [0001] The invention relates to the technical field of medicine preparation, in particular to a semicarbazone derivative used as a caspase-3 activator and its application in the preparation of medicines for treating and / or preventing cancer and other proliferative diseases. 【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] Apoptosis refers to an autonomous and orderly death process regulated by genes. It is generally believed that malignant transformation of tumo...

Claims

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Application Information

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IPC IPC(8): C07D417/12C07D417/14A61P35/00
CPCA61P35/00C07D417/12C07D417/14
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