Deuterium labelled 1-substituted phenyl-4-substituted anilinomethyl-1,2,3-triazole derivatives as well as preparation method and application thereof

Abstract

The invention relates to deuterium labelled 1-substituted phenyl-4-substituted anilinomethyl-1,2,3-triazole derivatives. The derivatives have the structure shown as general formula (I) in the description, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 can be -F, -Cl, -Br, -I, -OCD3, -NO2, -SO3D, -D, deuterium labelled alkyl groups with 1-18 carbon atoms, deuterium labelled substituted phenyl,deuterium labelled substituted benzyl or deuterium labelled heterocyclic substituents. The invention further discloses a preparation method of the derivatives and an application of the derivatives topreparation of tumor treating or preventing drugs. Compared with the prior art, the deuterium labelled 1-substituted phenyl-4-substituted anilinomethyl-1,2,3-triazole derivatives have the effect of inhibiting cancer cells, and are convenient to synthesize.

Description

technical field [0001] The invention belongs to the field of organic chemistry, and relates to an anticancer compound, in particular to a stable isotope deuterium-labeled 1-substituted phenyl-4-substituted anilinomethyl-1,2,3-triazole derivative and its preparation methods and applications. Background technique [0002] Cancer is a persistent disease that seriously endangers human health. Experts predict that it will become the number one killer that endangers human health and takes people's lives. Therefore, seeking high-efficiency and low-toxic anticancer drugs has become the goal of human unremitting efforts. [0003] Among the previous anticancer drugs, anticancer drugs are prone to drug resistance and often have adverse reactions, such as nausea, vomiting, fever and other symptoms, and are expensive, so the scope of use of anticancer drugs is very limited. [0004] In the early stage, Wang Zhonghua of Shanghai University of Technology and others disclosed a 1-substitut...

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Problems solved by technology

[0003] Among the previous anticancer drugs, anticancer drugs are prone to drug resistance and often have adverse reactions, such as nausea, vomiting, fever and other symptoms, and are expensive, so the scope of use of anticancer drugs is very limited

[0004] In the early stage, Wang Zhonghua of Shanghai University of Technology and others disclosed a 1-substituted phenyl-4-substituted anilinomethyl-1,2,3-triazole derivative and its preparation method and use in the patent CN104592133A, and synthesized a series of New compounds, tested for activity, but their activity is limited, about half of the compounds have a half inhibitory concentration IC50 greater than 200 μg / ml, basically no biological activity

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