CAS: 186392-40-5; Cp 91149

该化合物是一个属于小分子类别的化学化合物,主要被确认为具有选择性抑制某些蛋白色素的作用,因此对药物研究感兴趣,特别是在癌症治疗方面.该化合物显示与目标酶有特定联系,影响各种细胞信号路径.CP 91149的特点是独特的分子结构,有助于其生物活动.该物质通常在体外和活体中研究,以评估其功效和安全特征.与许多化学物质一样,处理CP 9149需要遵守安全议定书,因为其潜在的毒性和环境作用.其溶性,稳定性和再活动是影响其应用于研究和开发的重要因素.

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N,N-dimethylammonium chloride 5-chloro-1H-Indole-2-carboxylic acid (2S,3R)-3-amino-2-hydroxy-4-phenylbutanoic acid (2R,3R)-3-[(5-Chloro-1H-indole-2-carbonyl)-amino]-2-hydroxy-4-phenyl-butyric acid

合成工艺路线路线简述

    📜3(S),2(R)-N-[(1,1-Dimethylethoxy)Carbonyl]-3-Amino-2-Hydroxy-4-Phenylbutyronitrile置于盐酸,Sodium Hydroxide,1-羟基苯并三唑,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,三乙胺体系中,用 甲醇,二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 98.0H,反应生成5-氯-N-[(1S,2R)-3-(二甲基氨基)-2-羟基-3-氧代-1-(苯基甲基)丙基]-1H-吲哚-2-甲酰胺
    参考文献:人肝糖原磷酸化酶的吲哚-2-羧酰胺抑制剂.
    标题:人肝糖原磷酸化酶的吲哚-2-羧酰胺抑制剂.
    摘要:
    Doi:10.1021/jm980264K

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    专利信息


    专利号:US-11712432-B2
    优先权日:2018-12-20
    标题 :Method of treating cancer with an elevated glycogen content
    发明人：GENTRY MATTHEW S; SUN RAMON C; YOUNG LYNDSAY EA
    权利人:UNIV KENTUCKY RES FOUND
    摘要:A method of treating cancer is provided. The method includes administering to a subject in need thereof an effective amount of a compound selected from the group consisting of a glycogen phosphorylase inhibitor, a glycogen synthase inhibitor, a glycogen degradation molecule, an anti-sense oligonucleotide that down-regulates glycogen synthesis, and combinations thereof, where the cancer includes elevated levels of glycogen.

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    主要参考文献


    1: Gao N, Shang J, Huynh D, Manthati VL, Arias C, Harding HP, Kaufman RJ, Mohr I, Ron D, Falck JR, Lehrman MA. Mannose-6-phosphate regulates destruction of lipid-linked oligosaccharides. Mol Biol Cell. 2011 Sep;22(17):2994-3009. doi: 10.1091/mbc.E11-04-0286. Epub 2011 Jul 7.
    2: Yoshida T, Okuno A, Takahashi K, Ogawa J, Hagisawa Y, Kanda S, Fujiwara T. Contributions of hepatic gluconeogenesis suppression and compensative glycogenolysis on the glucose-lowering effect of CS-917, a fructose 1,6-bisphosphatase inhibitor, in non-obese type 2 diabetes Goto-Kakizaki rats. J Pharmacol Sci. 2011;115(3):329-35. Epub 2011 Feb 22. Epub 2007 Jun 20.
    5: Hampson LJ, Agius L. Increased potency and efficacy of combined phosphorylase inactivation and glucokinase activation in control of hepatocyte glycogen metabolism. Diabetes. 2005 Mar;54(3):617-23. Epub 2004 Aug 18. Epub 2004 Jan 16.

    合成参考文献


    参考文献:10.1074/jbc.m400431200
    摘要:Shang J, Lehrman MA. Activation of glycogen phosphorylase with 5-aminoimidazole-4-carboxamide riboside (AICAR). Assessment of glycogen as a precursor of mannosyl residues in glycoconjugates. J Biol Chem. 2004 Mar 26;279(13):12076–80. doi: 10.1074/jbc.m400431200.
    参考文献:10.1074/jbc.m405660200
    摘要:Green AR, Aiston S, Greenberg CC, Freeman S, Poucher SM, Brady MJ, Agius L. The Glycogenic Action of Protein Targeting to Glycogen in Hepatocytes Involves Multiple Mechanisms Including Phosphorylase Inactivation and Glycogen Synthase Translocation. Journal of Biological Chemistry. 2004 Nov;279(45):46474–82. doi: 10.1074/jbc.m405660200.
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