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喹啉类蛋白酪氨酸激酶抑制剂的研究进展 被引量：6

Progressed in quinolines as protein tyrosine kinase inhibitors
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摘要 蛋白酪氨酸激酶的过度表达与多种肿瘤的发生、发展及转移相关,抑制酪氨酸激酶活性可有效抑制肿瘤。目前已有11个小分子蛋白酪氨酸激酶抑制剂作为抗肿瘤药物上市,1个由美国FDA批准接受预登记的药物,超过100个候选药物处于临床试验阶段。其中喹唑啉结构的酪氨酸激酶抑制剂已成为临床上最常见的抗肿瘤化疗药物类别之一。综述了近年来与喹唑啉结构相似的具有喹啉骨架的酪氨酸激酶抑制剂研究进展。 Protein tyrosine kinases （ PTKs） are closely related with tumor progression. Compounds that inhibit the kinase activity of PTKs are potential chemotherapeutics to treat tumors. Eleven small molecular PTKs inhibitors as anticancer drugs have been approved by FDA. One small molecular has been approved to accept the registration of drugs and over 100 drug candidates are on clinical studies. Three 4-anilinoquinazolines are tyrosine kinase inhibitors （ TKIs） used in the treatment of certain types of cancer and the quinazolines have been of value in cancer chemotherapy. The current review article focuses on the progress of small molecular TKIs featuring a quinoline skeleton similar to the structrue of quinazoline.
作者 姜梦 刘丹 兰帅鹏
机构地区 沈阳化工大学制药与生物工程学院
出处 《化学试剂》 CAS CSCD 北大核心 2013年第4期333-336,346,共5页 Chemical Reagents
关键词 蛋白酪氨酸激酶 抑制剂 喹啉 抗肿瘤 protein tyrosine kinases inhibitor quinoline antitumor
分类号 R979.1 [医药卫生—药品]
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参考文献21

  • 1BILLER J A, BROOIJMAN S, WISSNER A, et al. Kinase domain mutations in cancer implications for small molecule drug design strategies [J]. J. Med. Chem. , 2009,52(6) :1 493-1 509.
  • 2BONOMI P. Clinical studies with non-iressa EGFR tyrosine kinase inhibitiors [ J ]. Lung. Cancer, 2003,41 ( 1 ) : 43-48.
  • 3EFLICHMAN C, HIDALGO M, BONI J P, et al. Phase I study of EKB-569,an irreversible inhibitor of the epidermal growth factor receptor in patients with advanced solid tumol's [ J ]. Clin. Oncol. , 2006,24 (15): 2 252-2 260.
  • 4KWARK E L, SORDELLA R, BELL D W, et al. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance gefitinib [ J ]. PANS, 2005,102 ( 21 ) : 7 665-7 670.
  • 5RABINDRAN S K,DISCAFANI C M,ROSORD E C,et al. Antitamor activity of HKI-272, an orally active irreversible inhibitor of the HER-2 tyrosine kinase [ J ]. Cancer Res. ,2004,64( 11 ) :3 958-3 965.
  • 6丛欣.多靶点抗肿瘤酪氨酸激酶抑制剂的研究进展[M].彭司勋.药物化学进展8.北京:化学工业出版社,2012:252-277.
  • 7DIANE H, YANONG D, WANG Fei-ye, et al. Synthesis and src kinase inhibitory activity of a series of 4-phenylamino-3-quinolinecarbonitriles [ J ]. Med. Chem. , 2001, 44:822 -833.
  • 8潘耀柱,白海,王存邦.酪氨酸激酶抑制剂抑制骨髓瘤细胞的增殖及黏附[J].中国现代医学杂志,2008,18(13):1863-1866. 被引量：2
  • 9CAO Xin, YOU Qi-dong, LI Zhi-yu, et al. Desigen and synthesis of 7-alkoxy-4-heteroaryl-amino-3-quinolinecar-bonitriles as dual inhibitors of c-Src kinase and nitric oxide synthase [J]. Bioorg. Med. Chem. , 2008,16 : 5 890-5 898.
  • 10MORPHY R. Selectively nonselective kinase inhibition: striking the right balance [ J ]. Med. Chem. , 2010,53 : 1 413-1 437.

二级参考文献9

  • 1FURSTOSS O, DOREY K, SIMON V, et al. c-Abl is an effector of Src for growth factor-induced c-myc expression and DNA synthesis[J]. EMBO J, 2002, 21(4): 514-524.
  • 2LEWIS JM, BASKARAN R, TAAGEPERA S, et al. Integrin regulation of c-Abl tyrosine kinase activity and cytoplasmic-nuclear transport[J]. Proc Natl Acad Sci USA, 1996, 24: 15174-15179.
  • 3WOODRING PJ, LITWACK ED, O'LEARY DD, et al. Modulation of the F-actin cytoskeleton by c-Abl tyrosine kinase in cell spreading and neurite extension [J]. J Cell Biol, 2002, 156: 879-892.
  • 4WOODRING PJ, HUNTER T, WANG JY, et al.Regulation of F-aetin-dependent processes by the Abl family of tyrosine kinases[J]. J Cell Sci, 2003, 116: 2613-2626.
  • 5HERNANDEZ SE, KRISHNASWAMI M, MILLER AL, et al. How do Abl family kinases regulate cell shape and movement?[J]. Trends Cell Biol, 2004, 14: 36-44.
  • 6DE VOS J, THYKJAER T, TARTE K, et al. Comparison of gene expression profiling between malignant and normal plasma cells with ligonucleotide arrays[J]. Oncogene, 2002, 21(44): 6848-6857.
  • 7DAMIANO JS, CRESS AE, HAZLEHURST LA, et al. Cell adhesion mediated drug resistance (CAM-DR): role of integrins and resistance to apoptosis in human myeloma cell lines [J]. Blood,1999, 93: 1658-1667.
  • 8QIANG YW, KITAGAWA M, HIGASHI M, et al. Activation of mitogen-activated protein kinase through alphaS/betal integrin is required for cell cycle progression of B progenitor cell line, Reh,on human marrow stromal cells[J]. Exp Hematol, 2000, 28(10): 1147-1157.
  • 9PENDERGAST AM. The Abl family kinases: mechanisms of regulation and signaling[J].Adv Cancer Res, 2002, 85: 51-100.

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化学试剂
2013年 第4期

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