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大环骨架在抗肿瘤药物研究开发中的应用

Macrocycles in Oncology Drug Discovery
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摘要 大环结构修饰位点多,并且本身具有多样性与新颖性。这些特点使得大环结构作为母核或者基本结构单元,正在药物研究开发中得到越来越广泛的应用。本文就近几年抗肿瘤药物研究开发中合成类大环化合物骨架的构建和修饰对靶点亲和力,靶点选择性及自身理化性质的影响作一综述。 The macrocyclic skeletons were emerging as important templates for medicinal chemists in the field of drug discovery, owning to their diverse modification points and their novelty. The effects of macrocyclization on potency, selectivity and physicochemical properties were mainly discussed, concentrating on recent case histories in oncology drug discovery.
作者 胡亮 周明 刘瑞环 余聂芳
机构地区 中南大学药学院分子设计与药物发现研究所
出处 《广州化工》 CAS 2013年第9期3-4,12,共3页 GuangZhou Chemical Industry
基金 国家自然科学基金项目(30873137 81172927)
关键词 大环骨架 结构修饰 抗肿瘤 新药开发 macrocycles structure modification anti - tumor drug discovery
分类号 R9 [医药卫生—药学]
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  • 1Driggers EM,Hale SP,Lee J,et al.The exploration of macrocycles fordrug discovery-an underexploited structural class [J],Nat.Rev.Drug-Discov.,2008,7(7):608-624.
  • 2Marsault E,Peterson ML.Macrocycles are great cycles:applications,opportunities,and challenges of synthetic macrocycles in drug discovery[J].J.Med.Chem.,2011,54(7):1961-2004.
  • 3Kwitkowski VE,Prowell TM,Ibrahim A,et al.FDA approval summary:temsirolimus as treatment for advanced renal cell carcinoma[ J].Oncol-ogist,2010,15(4):428-435.
  • 4Goodin S.Ixabepilone; a novel microtubule-stabilizing agent for thetreatment of metastatic breast cancer[ J] .Am.J.Health.Syst.Pharm.,2008,65(21):2017-2026.
  • 5Maroney AC,Marugan JJ,Mezzasalma TM,et al.Dihydroquinone ansa-mycins:toward resolving the conflict between low in vitro affinity andhigh cellular potency of geldanamycin derivatives [ J].Biochemistry,2006,45(17):5678-85.
  • 6Hart S,Goh KC,Novotny-Diermayr V,et al.SB1518,a novel macro-cyclic pyrimidine based JAK2 inhibitor for the treatment of myeloid andlymphoid malignancies[ J].Leukemia,2011,25(11):1751-1759.
  • 7William AD,Lee ACH,Goh KC,et al.Discovery of kinase spectrumselective macrocycle (16E)-14-methyl-20-oxa5 ,7,14,26-tet-raazatetracyclo[ 19.3.1.1(2,6).1(8,12 )] heptacosa-1 ( 25 ),2(26),3,5,8(27),9,11,16,21,23-decaene ( SB1317/TG02) ,apotent inhibitor of cyclin dependent kinases ( CDKs),janus kinase 2(JAK2),and Fms-like tyrosine kinase-3( FLT3 ) for the treatmentof cancer[J].J.Med.Chem.,2012,55( 1 ):169-196.
  • 8Spiegel J,Mas-Moruno C,Kessler H,et al.Cyclic aza-peptide inte-grin ligand synthesis and biological activity[ J].J.Org.Chem.,2012,77(12):5271-5278.
  • 9Huang Y,Strobel ED,Ho CY,et al.Macrocyclic BACE inhibitors:opti-mization of a micromolar hit to nanomolar leads [ J].Bioorg.Med.Chem..Lett.,2010,20(10):3158-3160.
  • 10Tao Z . F,Wang L,Stewart KD,et al.Structure-based design,synthe-sis,and biological evaluation of potent and selective macrocyclic check-point kinase 1 inhibitors[ J].J.Med.Chem.,2007 ,50(7):1514-1527.
广州化工
2013年 第9期

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