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Synthesis and Application of a Novel Antitumor Active Compound

A compound and tumor drug technology, applied in anti-tumor drugs, organic chemistry, drug combination, etc., can solve the problems of high cytotoxicity, no effect in advanced cancer, stronger than curative effect, etc.

Active Publication Date: 2021-12-07
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, for most cancer patients, the existing clinical anti-tumor drugs have a certain curative effect but at the same time have relatively high cytotoxicity. While inhibiting cancer cells, they will also inhibit the growth of normal cells in the normal body and produce side effects. Some The side effects are even stronger than the curative effect
In addition, in recent years, medical technology has only improved the effect of early cancer treatment, but has no effect on advanced cancer

Method used

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  • Synthesis and Application of a Novel Antitumor Active Compound
  • Synthesis and Application of a Novel Antitumor Active Compound

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Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0011] The present invention provides a kind of pyridothiophene compound, its structure is as shown in the following formula I:

[0012] Formula Ⅰ

[0013] The reaction for preparing the compounds described in the present invention is as follows:

[0014]

[0015] To prepare intermediate I, add tert-butyl 4-oxopiperidine-1-carboxylate (30.0 mmol), 2-cyanoacetamide (30.0 mmol) and sulfur (30.0 mmol) in absolute ethanol (200 mL) Morpholine (30.0 mmol). The resultant was refluxed for 8 hours. The suspension was cooled to ambient temperature and filtered through a pad of celite and washed with absolute ethanol (30 mL x 3). The combined filtrates were concentrated to dryness. The crude product was diluted with 95% ethanol (30 mL) and filtered to obtain a white solid product as shown in Formula I with a yield of 83%.

[0016] To prepare Intermediate II, to a solution of Intermediate I (10 mmol) and DIEA (20 mmol) in dichloromethane (60 mL) was added dropwise the correspond...

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Abstract

The invention relates to the synthesis and application of a novel antitumor active compound, belonging to the technical field of antitumor pharmacy. The technical problem to be solved by the present invention is to provide a compound that can resist but not limited to colorectal cancer cells. The compound includes the compounds shown below or pharmaceutically acceptable salts thereof. The compound of the present invention or a pharmaceutically acceptable salt thereof, said application is the application of a novel compound in the preparation of anticancer drugs, which has a certain inhibitory activity on tumor cells, especially HCT116 and Hep-G2, so as to be related The treatment of tumors provides new options. The compound of the invention has a simple structure and good activity, can be used as a leading compound of anticancer drugs, and has good application prospects. Formula Ⅰ

Description

technical field [0001] The invention relates to the field of anti-tumor related drugs. Specifically, the present invention relates to a compound with anti-tumor effect and its anti-tumor activity, and provides a preparation method to provide a basis for the development of drugs for the prevention and treatment of tumors. Background technique [0002] Cancer is one of the most harmful diseases to human life and health. A large number of people die from cancer every year. According to statistics, the total number of cancer deaths in the world reaches 7 million people every year. In my country, more than 1 million patients die from tumors every year. With the With the increase of population and the acceleration of population aging, the morbidity and mortality of tumors are also on the rise and have become the first cause of death of the urban population. The research and development of anticancer drugs has always been a hot spot in pharmaceutical research. [0003] At present, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D495/04A61P35/00
CPCA61P35/00C07D495/04
Inventor 何俊王贯罗小娇李蓉李峰
Owner SICHUAN UNIV