CAS: 10441-27-7; 3-Acetyl-7-Hydroxy-2H-Chromen-2-One

上下游产品

ethyl acetoacetate 2,4-Dihydroxybenzaldehyde 2-ethoxymethylene-3-oxobutanoic acid ethyl ester recorcinol bis[2,4-dihydroxybenzaldehyde]hydrazone 3-acetyl-7-phenyl-2H-chromen-2-one 3-acetyl-7-p-tolyl-2H-chromen-2-one

📜3-乙酰基-7-甲氧基香豆素置于aluminum (III) Chloride体系中,用 甲苯 用作溶剂,化学反应 3.0H,以68%的收率获得3-乙酰基-7-羟基-苯并吡喃-2-酮
参考文献:(6-和7-苯基)香豆素衍生物的合成及生物评价作为17β-羟基甾体脱氢酶1型的选择性非甾体抑制剂
标题:(6-和7-苯基)香豆素衍生物的合成及生物评价作为17β-羟基甾体脱氢酶1型的选择性非甾体抑制剂
摘要:17β-羟基类固醇脱氢酶1(17β-Hsd1)是一种酶,可催化nadph依赖性的弱雌激素雌酮还原为最有效的雌激素雌二醇,后者通过雌激素受体发挥增殖作用.17β-Hsd1在雌激素反应性组织中的过表达与激素依赖性疾病的发展有关,例如乳腺癌和子宫内膜异位症.因此,17β-Hsd1代表了开发新疗法的诱人靶标.我们发现,在重组酶分析中,简单的香豆素1和2可以显着抑制17β-Hsd1,对17β-Hsd2具有高选择性.我们假设引入了各种p-使用suzuki-Miyaura交叉偶联反应将香豆素核心的6或7位取代的苯基部分提供类固醇结构的模拟物,对17β-Hsd1的抑制作用得到改善.该系列中最好的抑制剂被证明是6A,Ic 50为270 Nm,对17β-Hsd1的选择性比对17β-Hsd2的要好,并且对α和β雌激素受体的选择性也很高.
Doi:10.1021/jm101104Z

专利信息

专利号:US-2023037284-A9
优先权日:2018-11-30
标题:Combination therapy of peptidomimetic macrocycles
发明人：GUERLAVAIS VINCENT; ANNIS DAVID ALLEN
权利人:AILERON THERAPEUTICS INC
摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.

专利号:US-2018371021-A1
优先权日:2017-05-11
标 题 :Peptidomimetic macrocycles and uses thereof
发明人：AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN
权利人:AILERON THERAPEUTICS INC
摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.

专利号:US-11091522-B2
优先权日:2018-07-23
标题 :Peptidomimetic macrocycles and uses thereof
发明人：AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN; ANNIS DAVID ALLEN
权利人:AILERON THERAPEUTICS INC
摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.

专利号:US-7041812-B2
优先权日:2001-08-29
标题 :Labeled nucleoside polyphosphates
发明人：KUMAR SHIV; SOOD ANUP
权利人:AMERSHAM BIOSCIENCES CORP
摘要:The present invention describes new compositions of matter in the form of labeled nucleoside polyphosphates with four or more phosphates. In addition compositions of nucleoside polyphosphates with four or more phosphates that are substrates for nucleic acid polymerases with enhanced substrate properties and methods of using these nucleoside polyphosphates for nucleic acid detection, characterization and quantification are described. The compositions provided by this invention include nucleoside polyphosphate, dideoxynucleoside polyphosphate, or deoxynucleoside polyphosphate analogues which have colorimetric, chemiluminescent, or fluorescent moieties, mass tags or an electrochemical tags attached to the terminal-phosphate. When a nucleic acid polymerase uses this analogue as a substrate, an enzyme-activatable label would be present on the inorganic polyphosphate by-product of phosphoryl transfer. Removal of the polyphosphate product of phosphoryl transfer via phosphate or polyphosphate transferring enzyme leads to a detectable change in the label attached thereon. When the polymerase assay is performed in the presence of a phosphatase, there is provided a convenient method for real-time monitoring of DNA or RNA synthesis and detection of a target nucleic acid.

专利号:US-7563574-B2
优先权日:2006-03-31
标题:Methods, systems and compositions for monitoring enzyme activity and applications thereof
发明人：KORLACH JONAS; TURNER STEPHEN
权利人:PACIFIC BIOSCIENCES CALIFORNIA
摘要:Methods of monitoring enzyme mediated reactions, and particularly nucleic acid synthesis reactions such as pyrosequencing methods that employ enzymatic reporter systems. The methods and systems provide elevated signal levels as compared to conventional pyrosequencing processes, and/or mediate de-phasing of sequencing analyses employing pyrosequencing or other “sequencing by synthesisâ€? methods.

专利号:CN-116444472-A
优先权日:2022-11-11
标 题 :Effective synthesis method of 7-hydroxy 3-methyl ketocoumarin