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辛二酰苯胺异差劲肟酸合成的实验设计

Experimental design of the synthesis of Suberoylanilide Hydroxamic Acid
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摘要 辛二酰苯胺异羟肟酸(Suberoylanilide Hydroxamic Acid,SAHA)是一种以组蛋白乙酰化修饰为作用靶点的新型抗肿瘤药。此文立足药学发展前沿,建立以辛二酸二乙酯为原料,经酯交换反应、苯胺酰胺化反应、羟胺胺解反应的三步合成方法,条件温和,安全性好,并选作本科生的药学综合性实验教学。 Suberoylanilide Hydroxamic Acid（SAHA） is a novel antitumor agent,which can inhibit the enzymatic activity of histone deacetylases.In this paper,based on the frontier development of Pharmacy,SAHA is synthesized from suberic acid diethyl ester by three steps of transesterification,amidation with aniline and aminolysis in hydroxylamine.With mild conditions and good security,this method has been used in teaching of undergraduate comprehensive pharmaceutical experiment.
作者 苏国琛 沈杰
机构地区 南开大学药学院
出处 《实验室科学》 2011年第1期68-69,72,共3页 Laboratory Science
关键词 辛二酰苯胺异羟肟酸 抗肿瘤药 药学综合实验 SAHA antitumor agent comprehensive pharmaceutical experiment
分类号 R914.5 [医药卫生—药物化学]
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参考文献10

  • 1FDA Approves.New Drug for Skin Cancer,Zolinza[EB/OL].http://www.fda.gov/bbs/topies/news/2006/new01484.htm1,2006-10-06.
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  • 7胡杨,陈国华,吴燕,杨尚彦.伏立诺他的合成[J].中国医药工业杂志,2009,40(7):481-483. 被引量：6
  • 8Sbardella EG,Massa S.Anew facile and expeditious synthesis of Nhydroxy-N'-phenyloct、-anediamide,a potent inducer of terminal cytodifferentiation[J].Org Prep Proced lnt,2001.33(4):391-394.
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二级参考文献34

  • 1Richon VM, Emiliani S, Verdin E, et al. A class of hybridpolar inducers of transformed cell differentiation inhibits histone deacetylases [J]. Proc Natl Acad Sci USA, 1998, 95 (6) : 3003-3007.
  • 2Mark PA. Discovery and development of SAHA as an anticancer agent [J]. Oncogene, 2007, 26 (9) : 1351-1356.
  • 3FDA Approves New Drug for Skin Cancer, Zolinza [EB/OL]. [2006-10-06]. http://www.fda.gov/bbs/topics/ news/2006/new01484.html.
  • 4Breslow R, Marks PA, Rifkind BA, et al. Novel potent inducers of terminal differentiation and methods of use thereof: WO, 9307148 [P]. 1993-04-15.
  • 5Stowell JC, Huot RI, van Voast L, et al. The synthesis of N-hydroxy-N'-phenyloctanediamide and its inhibitory effect on proliferation of AXC rat prostate cancer cells [J]. J Med Chem, 1995, 38(9): 1411-1413.
  • 6Sbardella EG, Massa S. A new facile and expeditious synthesis of N-hydroxy-N'-phenyloctanediamide, a potent inducer of terminal cytodifferentiation [J]. OrgPrep Proced lnt, 2001, 33 (4) : 391-394.
  • 7Gediya LK, Chopra P, Purushottamachar P, et al. A new simple and high-yield synthesis of suberoylanilide hydroxamic acid and its inhibitory effect alone or in combination with retinoids on proliferation of human prostate cancer cells [J]. J Med Chem, 2005, 48(15): 5047-5051.
  • 8Sakajiri S,Kumagai T,Kawamata N,et al.Histone deacetylase inhibitors profoundly decrease proliferation of human lymphoid cancer cell lines[J].Exp Hematol,2005,33(1):53-61.
  • 9Cohen LA,Marks PA,Rifkind RA,et al.Suberoylanilide hydroxamic acid (SAHA),a histone deacetylase inhibitor,suppresses the growth of carcinogen-induced mammary tumors[J].Anticancer Res,2002,22 (3):1497-1504.
  • 10Breslow R,Marks PA,Rifkind RA,et al.Novel potent inducers of terminal differentiation and methods of use thereof:WO,9307148[P].1993-04-15.(CA 1993,119:138765)

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2011年 第1期

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