多靶点酪氨酸激酶抑制剂的研究进展
Progress in the Research of Multi-Target Tyrosine Kinase Inhibitors
DOI: 10.12677/HJMCe.2016.44006, PDF, HTML, XML, 下载: 2,147  浏览: 7,619 
作者: 刘 丹, 李 雪, 张 毅, 彭鹏辉:沈阳化工大学,制药与生物工程学院,辽宁 沈阳
关键词: 多靶点酪氨酸激酶抑制剂抗肿瘤Multi-Target Tyrosine Kinase Inhibitor Antitumor
摘要: 多靶点酪氨酸激酶抑制剂的研究已经成为近年来抗肿瘤药物研究的新趋势。本文整合国内外相关文献,综述了近年来各课题组对不同结构的酪氨酸激酶抑制剂及抗肿瘤活性的研究进展,以期为酪氨酸激酶抑制剂的研究与开发提供参考。
Abstract: The study on multi-targeted tyrosine kinase inhibitors has become a new trend in researches on antitumor drugs in recent years. In order to offer reference to the research and development of tyrosine kinase inhibitors, this review introduced the research results of tyrosine kinase inhibitors with different structures and antitumor activity by summarizing related literature, at home and abroad.
文章引用:刘丹, 李雪, 张毅, 彭鹏辉. 多靶点酪氨酸激酶抑制剂的研究进展[J]. 药物化学, 2016, 4(4): 42-54. http://dx.doi.org/10.12677/HJMCe.2016.44006

参考文献

[1] 郭建军, 朱晶, 赵永跃, 等. 不可逆性酪氨酸激酶抑制剂的研究进展[J]. 中国药理学通报, 2015, 31(6): 749-754.
[2] 康从民, 赵绪浩, 于玉琪, 等. 吲哚衍生物类VEGFR-2酪氨酸激酶抑制剂的从头设计[J]. 高等学校化学学报, 2014, 35(3): 550-554.
[3] 宋艳宁, 张赫然, 尹东东, 等. 小分子酪氨酸激酶抑制剂在癌症靶向治疗的研究进展[J]. 中国药学杂志, 2016, 51(3): 165-169.
[4] 王乐, 李明春, 等. 表皮生长因子受体酪氨酸激酶抑制剂联合用药治疗非小细胞癌的研究进展[J]. 中国药理学与杂志, 2016, 51(3): 165-169.
[5] Giamas, G., Man, Y.L., Hirner, H., et al. (2010) Kinases as Targets in the Treatment of Solid Tumors. Cell Signal, 22, 984-1002. https://doi.org/10.1016/j.cellsig.2010.01.011
[6] 李文丽. 酪氨酸蛋白激酶抑制剂的设计、合成和筛选[D]: [硕士学位论文]. 吉林: 吉林大学药学系, 2014.
[7] 王勇, 龙亚秋. 蛋白酪氨酸激酶小分子抑制剂的研究新进展[J]. 有机化学, 2011, 31(10): 1595-1606.
[8] 茆勇军, 李海泓, 李剑峰, 等. 蛋白酪氨酸激酶信号转导途径与抗肿瘤药物[J]. 药学学报, 2008, 43(4): 323-334.
[9] 刘靖, 王林, 杨晓明, 等. 多靶点蛋白酪氨酸激酶抑制剂的研究进展[J]. 国际药学研究杂志, 2009, 36(3): 161- 163.
[10] Summy, J.M. and Gallick, G.E. (2006) Treatment for Advanced Tumors: SRC Reclaims Center Stage. Clinical Cancer Research, 12, 1398-1401.
[11] Schenone, S., Manetti, F. and Botta, M. (2007) SRC Inhibitors and Angiogenesis. Current Pharmaceutical Design, 13, 2118-2128.
[12] Weisberg, E., Manley, P.W. and Cowan-Jacob, S.W. (2007) Second Generation Inhibitors of BCR-ABL for the Treatment of Imatinib-Resistant Chronic Myeloid Leukaemia. Nature Reviews Cancer, 7, 345-356. https://doi.org/10.1038/nrc2126
[13] Schenone, S., Manetti, F. and Botta, M. (2007) Last Findings on Dual Inhibitors of abl and SRC Tyrosine-Kinases. Mini Reviews in Medicinal Chemistry, 7, 191-201.
[14] Cao, X., You, Q.D. and Li, Z.Y. (2008) Recent Progress of SRC Family Kinase Inhibitors as Anticancer Agents. Mini Reviews in Medicinal Chemistry, 8, 1053-1063.
[15] Diane, H.B. (2008) Exploitation of the 3-Quinolinecarbonitrile Template for SRC Tyrosine Kinase Inhibitors. Current Topics in Medicinal Chemistry, 8, 922-934.
[16] 张秋荣, 陈婷, 于康, 等. 多靶点蛋白酪氨酸激酶抑制剂类抗肿瘤药物的研究进展[J]. 海峡药学, 2012, 24(2): 8.
[17] 康从民, 代英杰, 王巧燕, 等. 小分子蛋白酪氨酸激酶抑制剂及其作用机制[J]. 中国新药杂志, 2013, 22(10): 1170-1172.
[18] 王洪波, 陈晓光, 等. EGFR抑制剂耐药机制研究的新进展[J]. 国际药学研究杂志, 2007, 34(5): 347-355.
[19] 王灵杰, 胡雅芳, 汪凤梅, 等. 多靶点酪氨酸激酶抑制剂的研究进展[J]. 中国药房,2013, 24(13): 1233-1235.
[20] 宋艳宁, 张赫然, 尹东东, 等. 小分子酪氨酸激酶抑制剂在癌症靶向治疗的研究进展[J]. 中国药学杂志, 2016, 51(3): 165-171.
[21] 张秋荣, 陈婷, 于康, 等. 多靶点蛋白酪氨酸激酶抑制剂类抗肿瘤药物的研究进展[J]. 海峡药学, 2012, 24(2): 7-10.
[22] 吴建楠, 宋萌. 非受体酪氨酸激酶对细胞功能的影响及其研究进展[J]. 实用医学杂志, 2015, 31(3): 339-340.
[23] Zhang, J., Yang, P.L. and Gray, N.S. (2009) Targeting Cancer with Small Molecule Kinase Inhibitors. Nature Reviews Cancer, 9, 28-39. https://doi.org/10.1038/nrc2559
[24] 李伟, 雷春花, 王立强, 等. 多靶点受体酪氨酸激酶抑制剂喹啉衍生物的合成及活性初步研究[J]. 中国新药杂志, 2016, 25(13): 1522-1530.
[25] Liu, D., Luan, T., et al. (2014) Advance in Search for Afatinib and Its Aalogues, the Multi-Target Tyrosine Kinae Inhibitor. Chinese Pharmaceutical Journal, 49, 2145-2149.
[26] Khan, I., Ibrar, A., Ahmed, W. and Saeed, A. (2015) Synthetic Approaches, Functionalization and Therapeutic Potential of Quinazoline and Quinazolinone Skeletons: The Advances Continue. European Journal of Medicinal Chemistry, 90, 124-169. https://doi.org/10.1016/j.ejmech.2014.10.084
[27] 黄庄霖. 喹唑啉结构的多靶点酪氨酸激酶抑制剂研究进展[J]. 海峡药学, 2011, 23(10): 22-24.
[28] Han, W., Pan, H., Chen, Y., et al. (2011) EGFR Tyrosine Kinase Inhibitors Activate Autophagy as a Ytoprotrctive Response in Human Lung Cancer Cells. PLoS ONE, 6, e18691. https://doi.org/10.1371/journal.pone.0018691
[29] Fukuoka, M., Yano, S., Giaccone, G., et al. (2003) Multi-Institutiongal Randomized Randomized PhaseⅡ Trial of Gefitinib for Previously Treated Patients with Advanced Non-Small-Cell Lung Cancer. Journal of Clinical Oncology, 21, 2237-2246.
[30] Kris, M.G., Natale, R.B., Herbst, R.S., et al. (2003) Efficacy of Gefitinib, an Inhibitor of the Epidermal Growth Factor Receptor Tyrosine Kinase, in Symptomatic Patients with Non-Small Cell Lung Cancer—A Randomized Trial. JAMA, 290, 2149-2158. https://doi.org/10.1001/jama.290.16.2149
[31] 王慧杰, 王燕, 张湘如, 等. Gefitinib靶向治疗非小细胞肺癌的现状与进展[J]. 癌症进展杂志, 2005, 3(2): 163- 169.
[32] Dong, Q.G. (2004) Epidermal Growth Factor Receptor Family and Molecular Targeting Therapy of Lung Cancer. Cancer, 24, 93-95.
[33] 李冬冬. 喹唑啉类化合物的设计, 合成及生物活性评价[D]: [博士学位论文]. 南京: 南京大学, 2014.
[34] Hu, E., Tasker, A., White, R.D., et al. (2008) Discovery of Aryl Aminoquinazoline Pyridones as Potent, Selective, and Orally Efficacious Inhibitors of Receptor Tyrosine Kinase C-Kit. Journal of Medicinal Chemistry, 51, 3065-3069. https://doi.org/10.1021/jm800188g
[35] Vanbrocklin, H.F., Lim, J.K., Coffing, S.L., et al. (2005) Anilinodialkoxyquinazolines: Screening Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors for Potential Tumor Imaging Probes. Journal of Medicinal Chemistry, 48, 7445-7456. https://doi.org/10.1021/jm050607w
[36] Al-Omary, F.A.M., Hassan, G.S., El-Messery, S.M., et al. (2012) Subsitituted Thiazoles V. Synthesis and Antitumor Activity of Novel Thiazolo [2,3-b] Quinazoline and Pyrido [4,3-d]Thiazolo[3,2-d] Pyrimidine Analogues. European Journal of Medicinal Chemistry, 47, 65-72 https://doi.org/10.1016/j.ejmech.2011.10.023
[37] HU, S.J., XIE, G.J., ZHANG, D.X., et al. (2012) Synthesis and Biological Evaluation of Crown Ether Fused Quinazoline Analogues as Potent EGFR Inhibitors. Bioorganic & Medicinal Chemistry Letters, 22, 6301-6305. https://doi.org/10.1016/j.bmcl.2012.06.067
[38] Jallal, H., Valentino, M.L., Chen, G., et al. (2007) A Src/Abl Kinase Inhibitor, SKI-606, Blocks Breast Cancer Invasion Growth and Metastasis in Vitro and in Vivo. Cancer Research, 67, 1580-1588. https://doi.org/10.1158/0008-5472.CAN-06-2027
[39] Dan, L., Tian, L., Jian, K., Ying, Z. and Hai, F.W. (2016) Synthesis and Anti-Tumor Activities of 4-Anilinoquinoline Derivatives. Molecules, 21, 21.
[40] Liu, F.Y. (2013) Discovery of a Selective Irreversible BMX Inhibitor for Prostate Cancer. ACS Chemical Biology, 8, 1423-1428. https://doi.org/10.1021/cb4000629
[41] Li, W., Lei, C.H., Wang, L.Q., et al. (2016) Synthesisi and Preliminary Research of Quinoline Derivatives as Multi- Targeted Receptor Tyrosine Inhibitors. Chinese Journal of New Drugs, 25, 1522-1529.
[42] Morphy, R. (2010) Selectively Nonselective Kinase Inhibition: Striking the Right Balance. Journal of Medicinal Chemistry, 53, 1413-1437. https://doi.org/10.1021/jm901132v
[43] 张晶, 程璐, 梁泰刚, 等. 苯酰胺类C-Met激酶抑制剂的合成及其体外抗肿瘤活性研究[J]. 现代药物与临床, 2016, 31(9): 1313-1318.
[44] 刘长春, 王天扬, 张雨晴, 等. 2-氨基-N-(2-氯-6-甲基苯基)噻唑-5-甲酰胺的合成[J]. 中国医药工业杂志, 2016, 47(7): 848-850.
[45] Gangjee, A., Kurup, S., Ihant, M.A., et al. (2012) N4-Aryl-6-Substitutedphenylmetyl-7-H-Pyrrol[2,3-d] Pyrimidine-2, 4-Diamine as Receptor Tyrosine Kinase Inhibitors. Bioorganic & Medicinal Chemistry, 20, 910-914. https://doi.org/10.1016/j.bmc.2011.11.058
[46] Lang, X., Sun, Q., Chen, Y., et al. (2013) Novel Synthetic 9-Benzyloxyacridine Analogue as Both Tyrosine Kinase and Topoisomerase l Inhibitor. Chinese Chemical Letters, 44, 661-665. https://doi.org/10.1016/j.cclet.2013.05.018