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含三氮唑基团的新型PI3K抗肿瘤抑制剂的设计与合成 被引量：1

Design and Synthesis of a Novel Series of Triazole-based PI3-kinase Inhibitors for the Treatment of Cancer
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摘要 以PI3K/Akt信号通路为靶标的小分子抑制剂的研究已成为抗肿瘤新药研究的热点。以GDC-0941为先导物,合成一系列含三氮唑基团的新型PI3K抗肿瘤抑制剂,并进行了体外抗肿瘤活性评价,期望从中筛选出活性优于GDC-0941的新型抗肿瘤候选药物。 The research of small molecule inhibitors targeting at PI3K/Akt singling pathway has become a hot spot for exploration of new anti-tumor drugs.GDC-0941 selected as a leading compound,a novel series of triazole-based PI3K inhibitors were synthesized and evaluated for their anti-proliferative activities in vitro to find novel candidates with more potent activity than GDC-0941.
作者 陈绍俊 方渡 樊后兴
机构地区 湖南中医药大学 上海阳帆医药科技有限公司
出处 《化工时刊》 CAS 2010年第5期15-19,77,共6页 Chemical Industry Times
关键词 PI3K 合成 含三氮唑基团抑制剂 抗肿瘤活性 Phosphatidylinositol-3-kinase（PI3K） synthesis triazole-Based Inhibitor anticancer activity
分类号 TQ464.8 [化学工程—制药化工]
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参考文献10

  • 1Vivanco I,Sawyers C L.The phosphatidylinositol 3-kinase AKT pathway in human cancer[J].Nat.Rev.Cancer 2002,2,489-501.
  • 2Vanhaesebroeck B,Leevers S J,Ahmadi K,Timms J,Katso R,Driscoll P C,Woscholski R,Parker P J,Waterfield M D.Synthesis and function of 3-phosphorylated inositol lipids[J].Annu.Rev.Biochem.2001,70,535-602.
  • 3Solit D B,Basso A D,Olshen A B,Scher H I,Rosen N.Inhibition of heat shock protein 90 function down-regulates Akt kinase and sensitizes tumors to Taxol[J].Cancer Res 2003,63,2139-2144.
  • 4Peng Wu,Tao Liu and Yongzhou Hu.PI3K Inhibitors for Cancer Therapy:What has been Achieved So Far?[J].Current Medicinal Chemistry,2009,16,916-930.
  • 5Samuels Y,Wang Z,Bardelli A.,et al.High frequency of mutations of the PIK3CA gene in human cancers[J].Science 2004,304(5670),554.
  • 6Adrian J,Folkes,Khatereh Ahmadi,Wendy K Alderton,Sonia Alix,Stewart J.The identification of 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-m-orpholin-4-yl-thieno[3,2-d] pyrimidine (GDC-0941) as a Potent,Selective,Orally Bioavailable Inhibitor of Class I PI3 Kinase for the Treatment of Cancer[J].J.Med.Chem.,2008,51 (18),5522-5532.
  • 7Woitun E,Ohnacker G,Narr B,Horch U,Kadatz R.U.S.Patent 3763156,1973.
  • 8Diane H Boschelli,Biqi Wu,Ana Carolina Barrios Sosa,Haris Durutlic,Fei Ye,Yuri Raifeld,Jennifer M Golas,Frank Boschelli.Identification of 7-Phenylaminothieno-[3,2-b] pyridine-6-carbonitriles as a New Class of Src Kinase Inhibitors[J].J.Med.Chem.2004,47,6666-6668.
  • 9Yufeng Chen,Miriam Lopez-Sanchez,Doris N Savoy,Daniel D Billadeau,Geoffrey S Dow,and Alan P Kozikowski.A series of potent and selective,triazolylphenyl-based histone deacetylases Inhibitors with activity against pancreatic cancer cells and plasmodium falciparum[J].J.Med.Chem.2008,51,3437-3448.
  • 10Mosmann T.Rapid colorimetric assay for cellular growth and survival:application to proliferration and cytotoxicity assays[J].J Immunol Methods,1983,65 (1-2),55-63.

同被引文献10

  • 1Carta A,Sanna P,Palomba M,et al.Synthesis and antiproliferative activity of 3-aryl-2-(1H-benzotriazol-1-yl)acrylonitriles PartIII[J].Eur J Med Chem,2002,37(11):891-900.
  • 2Carta A,Palomba M,Boatto G,et al.Synthesis and antiproliferative activity of 3-aryl-2-[1H(2H)-benzotriazol-1(2)-yl]acrylonitriles variously substituted:Part 4[J].Farmaco,2004,59(8):637-644.
  • 3Carta A,Palomba M,Paglietti G,et al.[1,2,3]Triazolo[4,5-h]quinolones.A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains[J].Bioorg Med Chem Lett,2007,17(17):4791-4794.
  • 4Wu C Y,King K Y,Kuo C J,et al.Stable benzotriazole esters as mechanism-based inactivators of the severe acute respiratory syndrome 3CL protease[J].Chem Biol,2006,13(3):261-268.
  • 5Whiting M,Tripp J C,Lin Y C,et al.Rapid discovery and structure-activity profiling of novel inhibitors of human immunodeficiency virus type 1 protease enabled by the copper(I)-catalyzed synthesis of 1,2,3-triazoles and their further functionalization[J].J Med Chem,2006,49(26):7697-7710.
  • 6Giffin M J,Heaslet H,Brik A,et al.A copper(I)-catalyzed 1,2,3-triazole azide-alkyne click compound is a potent inhibitor of a multidrug-resistant HIV-1 protease variant[J].J Med Chem,2008,51(20):6263-6270.
  • 7Cho J H,Bernard D L,Sidwell R W,et al.Synthesis of cyclopentenyl carbocyclic nucleosides as potential antiviral agents against orthopoxviruses and SARS[J].J Med Chem,2006,49(3):1140-1148.
  • 8Kallander L S,Lu Q,Chen W,et al.4-Aryl-1,2,3-triazole:a novel template for a reversible methionine aminopeptidase 2 inhibitor,optimized to inhibit angiogenesis in vivo[J].J Med Chem,2005,48(18):5644-5647.
  • 9Reck F,Zhou F,Girardot M,et al.Identification of 4-substituted 1,2,3-triazoles as novel oxazolidinone antibacterial agents with reduced activity against monoamine oxidase A[J].J Med Chem,2005,48(2):499-506.
  • 10叶晓,许秀枝,王艰,李柱来.1(2)-N-乙腈基取代苯并三氮唑合成条件的研究[J].福建医科大学学报,2010,44(2):112-115. 被引量：5

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化工时刊
2010年 第5期

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