CAS: 20797-48-2; 3-(4-Chloro-3-Nitrophenyl)Acrylic Acid

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CAS号30565-73-2 α,p-Dichlor-m-n... | CAS号55912-20-4 4-氯-3-硝基苯甲醇 | CAS号1615-02-7 4-氯肉桂酸 | CAS号7697-37-2 硝酸

丙二酸,4-氯-3-硝基苯甲醛置于哌啶,吡啶体系中,化学反应 2.5H,以82.1%的收率获得4-氯-3-硝基肉桂酸
参考文献:具有异羟肟酸结构的化合物及其制备方法和应用
标题:具有异羟肟酸结构的化合物及其制备方法和应用
摘要:本发明提供了具有异羟肟酸结构的化合物及其制备方法和应用,属于化学药物领域.本发明提供的具有异羟肟酸结构的化合物,具有如式i,ⅱ或ⅲ所示的化学结构,通过将刺猬信号通路拮抗剂的药效基团与异羟肟酸片段拼合,增加化合物与hdac中锌离子的螯合作用,在保持对刺猬信号通路拮抗作用的同时表现出较强的hdac抑制作用.本发明提供的具有异羟肟酸结构的化合物,在浓度为10μm时,对hdac的抑制率高达93.43%,在浓度为5μm时,下调刺猬信号通路转录因子gli1的表达可达到‑87.10%,表现出对刺猬信号通路的活性有较强的抑制作用,在浓度为10μm时,对a549非小细胞肺癌细胞增殖的抑制率高达86.84%,抑制jurkat白血病细胞的ic50值低至0.57μm.

专利信息

专利号:US-9217012-B2
优先权日:2009-04-08
标题 :Inhibitors of protein tyrosine phosphatases
发明人：ZHANG ZHONG-YIN; ZHANG SHENG
权利人:ZHANG ZHONG-YIN; ZHANG SHENG; UNIV INDIANA RES & TECH CORP
摘要:Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.