CAS: 16800-67-2; 1-[3-(Acetyloxy)-1H-Indol-1-Yl]Ethanone

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📜2-溴苯甲酸置于乙酸酐,铜,Potassium Carbonate,Potassium Hydroxide体系中,用 水 用作溶剂,化学反应 17.0H,反应生成N,O-1,3-二乙酰基吲哚
参考文献:靛玉红衍生物作为靶向细胞周期蛋白依赖性激酶和组蛋白脱乙酰酶的双重抑制剂用于治疗癌症
标题:靛玉红衍生物作为靶向细胞周期蛋白依赖性激酶和组蛋白脱乙酰酶的双重抑制剂用于治疗癌症
摘要:为了利用天然产物靛玉红的独特支架,我们在此采用组合药效团的策略来设计和合成一系列新型靛玉红衍生物,作为针对细胞周期蛋白依赖性激酶 (Cdk) 和组蛋白脱乙酰酶 (Hdac) 的双重抑制剂.其中,先导化合物8B具有显着的cdk2/4/6和hdac6抑制活性,Ic 50 = 60.9 +/-2.9,276 +/-22.3,27.2 +/-4.2和128.6 +/-0.4 Nm,可有效诱导细胞凋亡和s期在几种癌细胞系中停滞.特别是化合物8B可以通过 Mcl-1/xiap/parp 轴阻止非小细胞肺癌细胞系 (A549) 的增殖,这与 Hdac 抑制剂和 Cdk 抑制剂联合药物的独特作用模式一致.在 A549 静电复印机模型中,化合物8B显示出与其双重抑制相关的显着抗肿瘤功效.我们的数据表明,化合物8B作为单一药物可能是与 Cdk 和 Hdac 抑制剂联合用于癌症治疗的有希望的候选药物.
Doi:10.1021/acs.Jmedchem.1C01311

专利信息

专利号:US-6844346-B2
优先权日:1997-10-27
标 题 :Chromogenic substrates of sialidase and methods of making and using the same
发明人：JOHNSON STEPHEN C; SAEED ASHRAF; LUO MING
权利人:IBBEX INC; UNIV OF ALABAMA AT BIRMINGHAM
摘要:The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including humans) origin. These compounds are based upon N-acetylneuraminic acid glycosides. In particular, this invention provides a novel class of these compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.

专利号:US-6667161-B1
优先权日:1997-10-27
标 题 :Chromogenic substrates of sialidase of bacterial, viral, protozoa, and vertebrate origin and methods of making and using the same
发明人：JOHNSON STEPHEN C; LOU MING; YAN SHIJIA
权利人:IBBEX INC; UAB RESEARCH FOUNDATION
摘要:The current invention relates to the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including human) origin. In particular, this invention provides a novel class of effective compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.

专利号:US-5925647-A
优先权日:1995-06-07
标 题 :Methods for use of cryptolepine analogs with hypoglycemic activity
发明人：BIERER DONALD E
权利人:SHAMAN PHARMACEUTICALS INC
摘要:Novel cryptolepine analogs useful as hypoglycemic agents and methods for their use as hypoglycemic agents, for example, in the treatment of diabetes, and a method for their synthesis are described. As hypoglycemic agents, the novel cryptolepine analogs are useful for the treatment of insulin-dependent diabetes mellitus (IDDM or Type I) and non-insulin dependent diabetes mellitus (NIDDM or Type II).

专利号:WO-2024231384-A1
优先权日:2023-05-10
标题:Compositions for treating senescence related disease
发明人：PENDE MARIO; FUMAGALLI STEFANO
权利人:INST NAT SANTE RECH MED; CENTRE NAT RECH SCIENT; UNIV PARIS CITE
摘要:Inventors have identified glycerol-3-phosphate (G3P) and phosphoethanolamine (PEtn) metabolism as potent regulators of the senescent program at the nexus of TAG and PL metabolism. They show that Glycerol kinase (GK) and Phosphate Cytidylyltransferase 2 Ethanolamine (Pcyt2) activities, which catalyse regulatory steps in TAG and PL synthesis impact G3P and PEtn levels in a homeostatic fashion controlling the senescence program. Finally, they provide evidence that pharmacological inhibitors of GK activity act senomorphic, thus suggesting a novel therapeutic target for interventions in age-related diseases and cancer. The present invention relates to a method for treating senescence related disease in a subject in need thereof comprising administering said subject with a therapeutically effective amount of a modulator of Glycerol kinase (GK), Glycerol 3 phosphate phosphatase (G3PP), Ethanolamine-Phosphate Phospho-Lyase (ETNPPL) and/or Phosphate Cytidylyltransferase 2 (PCYT2).

专利号:WO-9610015-A1
优先权日:1994-09-28
标题 :Cryptolepine analogs with hypoglycemic activity
发明人：BIERER DONALD E
权利人:SHAMAN PHARMACEUTICALS INC
摘要:Novel cryptolepine analogs useful as hypoglycemic agents and methods for their use as hypoglycemic agents, for example, in the treatment of diabetes, and a method for their synthesis are described. As hypoglycemic agents, the novel cryptolepine analogs are useful for the treatment of insulin-dependent diabetes mellitus (IDDM or Type I) and non-insulin dependent diabetes mellitus (NIDDM or Type II).

专利号:WO-9845272-A1
优先权日:1997-04-07
标题:Topoisomerase inhibitors
发明人：DEADY LESLIE WILLIAM; DENNY WILLIAM ALEXANDER; KAYE ANTHONY JAMES
权利人:UNIV LATROBE; DEADY LESLIE WILLIAM; DENNY WILLIAM ALEXANDER; KAYE ANTHONY JAMES
摘要:The invention provides a novel series of tetracyclic quinoline and quinoxaline carboxamides, bis compounds in which two of the tetracyclic compounds are joined by a linker, and pharmaceutically-acceptable salts and N-oxides thereof, which have the ability to inhibit topoisomerase activity. The compounds are active in vitro and in vivo against tumour cells. Methods of synthesis and pharmaceutical compositions are also claimed.