Tert-butyl substituted asymmetrical piperidone compounds with anti-tumor activities and preparation method thereof

Abstract

The invention relates to six tert-butyl substituted asymmetrical piperidone compounds with anti-tumor activities and a preparation method thereof, and belongs to the technical field of anti-tumor medicaments and a preparation method thereof. According to the preparation method, a Claisen-Schmidt condensation reaction is performed on N-methyl-4-piperidone, 4-tert-butylbenzaldehyde and another aromatic aldehyde to obtain products A-F. The compounds have high anti-tumor activities, genotoxicity of the conventional anti-tumor medicaments can be avoided, and the toxicity to normal cells is low. The preparation method is easy and convenient to operate, is mild in the reaction condition, is high in synthesis yield, and can be widely popularized in the anti-tumor field.

Description

technical field

[0001] The invention relates to a series of tert-butyl substituted asymmetric piperidone compounds with antitumor activity and a preparation method thereof, belonging to the technical field of antitumor drugs and preparation methods thereof. Background technique

[0002] 3,5-diaryl methylene-4-piperidone derivatives belong to curcumin analogs, which contain two α,β-unsaturated ketone pharmacophores, which can inhibit the higher content of tumor cells Sulfhydryl has a strong affinity, thus exhibiting superior antitumor activity [1] . Compared with clinical anti-tumor drugs, it has two advantages: first, as a cytotoxic drug, it can effectively avoid the genotoxicity of current clinical chemotherapy drugs, and the experimental verification that the mechanism of cell apoptosis may be through the activation of caspase3 to induce internucleosomal DNA It is also confirmed by experiments that it induces cell autophagy; the second is that the molecule contains two α...

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