Alpha-aryl-gamma-methylene butene lactone compounds, and synthesis method and application thereof

By developing α-aryl-γ-methylene butenolide compounds as new small molecule tubulin inhibitors, the problem of poor therapeutic effect of existing anti-tumor drugs has been solved, and the treatment of various tumor cells has been achieved. The effective inhibition has the potential to develop new anti-tumor drugs and simplify the synthesis process.

CN102827116AInactive Publication Date: 2012-12-19ZHENGZHOU UNIV
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Patent Information

Application Number
CN201210358666.5
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2012-09-25
Publication Date
2012-12-19
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

Existing anti-tumor drug treatments have not completely solved the cause of malignant tumors, resulting in a continued increase in tumor incidence and deaths, and there is a lack of effective new small molecule anti-tumor drugs.

Method used

A class of α-aryl-γ-methylene butenolide compounds were developed as new small molecule tubulin inhibitors. The compounds were prepared through a specific synthesis method and used as anti-tumor drugs. The method includes a multi-step reaction process, using different solvents, acid binding agents, bases, alkylating reagents, etc. to synthesize compounds.

Benefits of technology

The prepared compound shows good anti-tumor activity, has an inhibitory effect on a variety of tumor cells, has the potential to develop anti-tumor drugs with new mechanisms of action, and has a simple synthesis method and a high yield.

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Abstract

The invention discloses alpha-aryl-gamma-methylene butene lactone compounds, and a synthesis method and application thereof. The alpha-aryl-gamma-methylene butene lactone compounds has the following structural general formula (Formula 1), wherein R1 is hydrogen, monosubstituted or polysubstituted methyl group, methoxy group, fluorine, chlorine, bromine, hydroxy group, amino group, trifluoromethyl or the like; R2 is OR3 or NR4R5; R3 is C1-5 alkyl group; and R4 and R5 are respectively N or O containing five-element or six-element heterocyclic group, benzylamino group or the like. The compounds are a novel micromolecular tubulin inhibitor which has favorable inhibiting action on multiple tumor cells; and therefore, the compounds can be used for preparing antineoplastic drugs, and has the potential for developing antineoplastic drugs with novel acting mechanisms.
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