Hydroxamic acid compound, and preparation method and application thereof

A compound, hydroxamic technology, applied in the field of hydroxamic acid, can solve the problems of toxic reaction, HDACs subtype selectivity, poor bioavailability, etc., to achieve mild reaction conditions, affect cell cycle arrest, and few steps Effect
CN103159646AInactive Publication Date: 2013-06-19GUANGDONG PHARMA UNIV
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
GUANGDONG PHARMA UNIV
Publication Date
2013-06-19
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to the application areas of organic chemistry, pharmaceutical chemistry and medicine, and particularly discloses hydroxamic acid. The hydroxamic acid compound has a structure shown in Formula I, wherein R is selected from a substituted benzene ring, a heterocyclic ring, a substituted heterocyclic ring, a benzoheterocyclic ring or a substituted benzoheterocyclic ring, wherein the substitution refers to that 1-n hydrogen atoms on the benzene ring, heterocyclic ring or benzoheterocyclic ring are substituted by the following groups: halogen, amino, hydroxy, nitro, cyano, alkoxy, aminoalkyl, alkylamino, sulfoalkyl, perfluoroalkyl, perfluoroalkoxy, amido or alkoxycarbonyl. According to the invention, the hydroxamic acid compound achieves the purpose of treating neoplastic diseases by regulating histone deacetylase; the hydroxamic acid compound has anti-proliferation effect on tumor cells, influences cell cycle arrest and induces cell apoptosis; and above all, the anti-proliferation effect on lung cancer cell strains is obviously improved in comparison with the effect of a positive control drug SAHA (suberoylanilide hydroxamic acid).
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Description

technical field

[0001] The present invention relates to the field of organic chemistry, medicinal chemistry and medical application, more specifically, relates to a kind of isohydroxy

[0002] Oxymesic acid compounds and their preparation methods and applications. Background technique

[0003] In recent years, histone deacetylase inhibitors (histone deacetylase inhibitors, HDACi) have become one of the research hotspots of anti-tumor drugs. Currently, HDACi mainly include hydroxamic acids, cyclic tetrapeptides, short-chain fatty acids, benzamides, electrophilic ketones, and trithiocarbonic acids. Among them, the hydroxamic acid HDACi is the earliest discovered and the most extensively studied so far. It has strong enzyme inhibitory effect, simple structure and easy synthesis. Understanding the structure-activity relationship of hydroxamic acids is the key to design SAHA derivatives. The structure of this type of HDACi is mostly composed of ring, aliphatic chain and hydrox...

Claims

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