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以VEGFR为靶点的小分子抗肿瘤药物的研究进展 被引量：3

Advancement in antitumor angiogenesis:small molecular inhibitors of VEGFR
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摘要 人血管内皮生长因子受体(VEGFR)小分子抑制剂是一种新型的抗癌药物。近年来,发现了一些对VEGFR具有高选择性的化合物,并且有关这些化合物的设计、结构改造及药理活性的研究也取得了很大的进展。该文从结构类型的角度综述作用于VEGFR的单靶点和多靶点小分子抑制剂的最新研究进展,并简要总结了这些化合物的构效关系。 Inhibition of VEGFR signaling pathway has become a valuable approach in the treatment of can-cers.In the past few years,some high selectivity compounds have been developed,which have made a great process on their design,structure modification and pharmacological research.In this review,the latest progress on the different chemical types of small-molecule inhibitors of VEGFR was reviewed.Meanwhile,the structure-activity relationship of these compounds was also summarized.
作者 胡国栋 杨千姣 景云荣 刘丹 赵临襄
机构地区 教育部基于靶点的药物设计与评价重点实验室
出处 《中国药物化学杂志》 CAS CSCD 2010年第5期434-441,共8页 Chinese Journal of Medicinal Chemistry
基金 国家科技部重大科技专项(2009ZX09103-080)
关键词 VEGFR小分子抑制剂 单靶点抑制剂 多靶点抑制剂 构效关系 抗肿瘤药物 small-molecule inhibitor of VEGFR selectively non-selective kinase inhibitor controlled multitarget therapy structure-activity relationship antitumor drug
分类号 R979.1 [医药卫生—药品]
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参考文献26

  • 1ZUCCOTTO F, ARDINI E, CASALE E, et al. Through the "gatekeeper door" :exploiting the active kinase konformation[ J ]. J Med Chem, 2010,53 ( 7 ) : 2681 - 2694.
  • 2PHILIP A H,BOLOOR A,CHEUNG M,et al. Discovery of 5-[ [ 4-[ ( 2,3-dimethyl-2H-indazol-6-yl ) methylamino ]-2-pyrimidinyl ] amino ]-2-methylbenzenesulfonamide(pazopanib) :a novel and potent vascular endothelial growth factor receptor inhibitor [ J ]. J Med Chem, 2008,51 ( 15 ) :4632 - 4640.
  • 3POTASHMAN M H, BREADY J, COXON A, et at. Synthesis, and evaluation of orally active benzimidazoles and benzoxazoles as vascular endothelial growth factor-2 receptor tymsine kinase inhibitors [J]. J Med Chem,2007,50(18) :4351 -4373.
  • 4HODOUS B L, HUGHES G-M, PAUL E H, et al. Structural analysis, and SAR studies of triazine deri- vatives as potent, selective Tie-2 inhibitors [ J ]. B ioorg Med Chem Lett,2007,17 (10) :2886- 2889.
  • 5HARMANGE C,WEISS M M. Naphthamides as novel and potent vascular endothelial growth factor re- ceptor tyrosine kinase inhibitors : design, synthesis, and evaluation [ J ]. J Med Chem, 2008, 51 ( 6 ) : 1649 - 1667.
  • 6WEISS M M, HARMANGE J-C, POLVERINO A J, et al. Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors [ J ]. J Med Chem,2008,51 (6) : 1668 - 1680.
  • 7LAD S,BELZILE J,BREADY J V,et al. Novel 2, 3-dihydro-1,4-benzoxazines as potent and orally bio- available inltibitors of tumor-driven angiogenesis [ J ]. J Med Claem ,2008,51 ( 6 ) : 1695 - 1705.
  • 8ANTHONY B D, PAUL B T, RYANC J, et al. Imidazo[ 1,2-a]pyridine compounds as VEGFR-2 inhibitots :WO,2006/091617 [ P]. 2006 - 08 - 31.
  • 9KISELYOV A S, MILLIGANB D, OUYANG X. Novel inhibitors of VEGF receptors-1 and -2 based on azole-5-carboxamide templates [ J ]. Bioorg Med Chem Lett ,2007,17 ( 13 ) :3550 - 3557.
  • 10BHIDE R S, MARINIER A. Pyrrol-pyridine kinase inhibitors : WO,2008/060907 [ P ]. 2008 - 05 - 22.

二级参考文献34

  • 1[1]Ciardiello F,Caputo R,Bianco R,et al.Inhibition of growth factor production and angiogenesis in human cancer cells by ZD1839 (Iressa),a selective epidermal growth factor receptor tyrosine kinase inhibitor.Clin Cancer Res,2001,7:1459
  • 2[2]Bruns C J,Solorzano CC,Harbison MT,et al.Blockade of the epidermal growth factor receptor signaling by a novel tyrosine ki nase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma.Cancer Res,2000,60:2926
  • 3[3]Wedge SR,Ogilvie DJ,Dukes M,et al.ZD6474 inhibits vascular endothelial growth factor signaling, angiogenesis,and tumor growth following oral administration.Cancer Res,2002,62:4645
  • 4[4]Wedge SR,Ogilvie,Dukes M,et al.Pharmacological efficacy of ZD6474,aVEGF receptor tyrosine kinase inhibitor,in rat. (Abstract) Proceedings of the 92nd Annal Meeting of the Ameri cian Association for Cancer Research,New Orleans (LA), 2001,42:Abst3126,583
  • 5[5]Wedge SR,Checkley D,Tessier JJ,et al.Dynamic contrast -enhanced MRI study of human xenografts treated with the VEGF signaling inhibitor ZD6474.Proceedings of the 92nd Annu al Meeting of the American Association for Cancer Research, New Orleans (LS),2001,42:Abst 581,107
  • 6[6]Manie S,Santoro M,Fusco A,et al.The RET receptor: Function in development and dysfunction in congenital malforma tion.Trends Genet,2001,17:580
  • 7[7]Carlomagno F,Vitagliano D,Guida T,et al.ZD6474,an orally available inhibitor of KDR tyrosine kinase activity,effi ciently blocks oncogenic RET kinases.Cancer Res,2002,62: 7284
  • 8[8]Ciardiello F,Caputo R,Damiano V,et al.Antitumor effects of ZD6474,a small molecule vascular endothelial growth factor receptor tyrosine kinase inhibitor,with additional activity against epidermal growth factor receptor tyrosine kinase.Clin Cancer Res,2003,9:1546
  • 9[9]Bruns C J,Kohl G,Guba M,et al.Anti-angiogenic and anti -tumor activity of a novel VEGFR-2 tyrosine kinase inhibitor ZD6474 in a metastatic human pancreatic tumor model.Proc Am Assoc Cancer Res (2nd ed),2003,44:604
  • 10[10]Williams KJ,Telfer BA,Brave S,et al.ZD6474,a potent inhibitor of vascular endothelial growth factor signaling,com bined with radiotherapy:Schedule-dependent enhancement of antitumor activity.Clin Cancer Res,2004,10:8587

共引文献21

同被引文献29

  • 1祁少海,沈锐,谢举临,刘坡,徐盈斌,利天增.以血管内皮生长因子受体为靶点抑制瘢痕血管增生的研究[J].中华实验外科杂志,2005,22(4):421-423. 被引量：13
  • 2刘刚,韩存芝.血管内皮生长因子及其受体与胶质瘤[J].肿瘤研究与临床,2006,18(9):640-643. 被引量：5
  • 3全欣,张燕,贾兵,赵慧云,余子璘,史纪云,王凡.^(99)Tc^m-HYNIC-β-Ala-BBN(7-14)NH_2的制备及其初步生物分布[J].同位素,2007,20(2):77-82. 被引量：1
  • 4Backer M V,Levashova Z,Patel V,et al.Molecular imaging of VEGFreceptors in angiogenic vasculature with single-chain VEGF-basedprobes[J].Nat Med,2007,13(4):504-509.
  • 5Ivy S P,Wick J Y,Kaufman B M.An overview of small-molecule in-hibitors of VEGFR signaling[J].Nat Rev Clin Oncol,2009,6(10):569-579.
  • 6Hsu A R,Cai W,Veeravagu A,et al.Multimodality molecular ima-ging of glioblastoma growth inhibition with vasculature-targeting fusiontoxin VEGF121/rGel[J].J Nucl Med,2007,48(3):445-454.
  • 7Rao P S,Thakur M L,Pallela V,et al.99Tcm labeled VIP analog:e-valuation for imaging colorectal cancer[J].Nucl Med Biol,2001,28(4):445-450.
  • 8Jia H,Jezequel S,Lohr M,et al.Peptides encoded by exon 6 ofVEGF inhibit endothelial cell biological responses and angiogenesis in-duced by VEGF[J].Biochem Biophys Res Commun,2001,283(1):164-173.
  • 9Qin Z X,Li Q W,Liu G Y,et al.Imaging targeted at tumor with(188)Re-labeled VEGF(189)exon 6-encoded peptide and effects ofthe transfecting truncated KDR gene in tumor-bearing nude mice[J].Nucl Med Biol,2009,36(5):535-543.
  • 10Liu W,Xu J,Wang M,et al.Tumor-derived vascular endothelialgrowth factor(VEGF)-a facilitates tumor metastasis through theVEGF-VEGFR1 signaling pathway[J].Int J Oncol,2011,39(5):1213-1220.

引证文献3

二级引证文献2

中国药物化学杂志
2010年 第5期

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