喹唑啉类表皮生长因子受体酪氨酸激酶抑制剂药物设计策略

doi:10.19286/j.cnki.cci.2021.05.042

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Abstract

Overexpression and mutation of epidermal growth factor play an important role in the formation and development of tumors. Treatment of tumors can be achieved by inhibiting epidermal growth factor receptor-mediated signal transduction. Quinazoline small molecule targeting epidermal growth factor receptor tyrosine kinase inhibitor drugs are one of the more active research fields, and many drugs have been marketed. Quinazoline derivatives have many structural modification sites and have strong market development potential. The development history of quinazoline epidermal growth factor receptor tyrosine kinase inhibitors, the synthesis methods of representative drugs, and the structure-activity relationship of drugs were reviewed, and the research prospect of quinazoline drugs was predicted based on the structure-activity relationship.

Key words： quinazoline small molecule targeting drugs epidermal growth factor receptor tyrosine kinase inhibitors tumor

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	Articles by authors
	Zhao Yongjie
	Meng Jian
	Hu Ruijuan
	Qie Zhenggang

Cite this article:

Zhao Yongjie,Meng Jian,Hu Ruijuan等. Drug design strategy for quinazoline epidermal growth factor receptor tyrosine kinase inhibitors[J]. CCI, 2021, 44(5): 138-141.

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http://www.mtyhg.com.cn/EN/10.19286/j.cnki.cci.2021.05.042 OR http://www.mtyhg.com.cn/EN/Y2021/V44/I5/138

[ 1 ]       Ruenraroengsak P, Cook J M, Florence A T. Nanosystem drug tar-
geting: facing up to complex realities[ J ]. J Con Rel, 2010, 141( 3 ): 265 - 276.
[ 2 ]       Robinson D R, Wu Y M, Lin S F. The protein tyrosine kinase fam-
ily of the human genome[ J ]. Oncogene, 2000, 19( 49 ): 5 548 - 5 557.
[ 3 ]       Lemmon M A, Schlessinger J. Cell signaling by receptor tyrosine
kinases[ J ]. Cell, 2010, 141( 7 ): 1 117 - 1 134.
[ 4 ]       Moslehi J J, Deininger M. Tyrosine kinase inhibitor-associated ca-
rdiovaseular toxicity in chronic myeloid leukemia[ J ]. JClin Oncol, 2015, 33( 35 ): 4 210 - 4 218.
[ 5 ]       Ciardiello F, De Vita F, Orditura M, et al. Epidermal growth factor receptor tyrosine kinase inhibitoes in late stage clinical[ J ]. Exp Opin Emerg Drugs, 2003（ 8 ）: 501 - 514.
[ 6 ]       Fry D W, Kraker A J, McMichael A, et al. A specific inhibitor of the novel epidermal growth factor receptor tyrosine kinase[ J ]. Science, 1994, 265(5 175): 1 093 - 1 095.
[ 7 ]       Tan F, Shi Y, Wang Y, et al. Icotinib a selective EGF receptor tyr-
osine kinase inhibitor, for the treatment of non-small-cell lung eancer[ J ]. Future Oncol, 2015,11( 3 ): 385 - 397.
[ 8 ]       张    华，赵金浩，王    晖. 4-（3-氯-4-氟苯氨基）-7-甲氧基-6-[3-（4-吗啉基）-丙氧基]喹啉的合成法：CN101402610A[ P ].
[ 9 ]       李文倩，宋国强，万屹东，等. 阿法替尼的合成工艺改进[ J ]. 合成化学，2017，25（ 2 ）：166 - 169.
[ 10 ]     许学农. 阿法替尼的制备方法：中国，CN201310182778. 4[ P ].
[ 11 ]     Yu H A, Tian S K, Drilon A E, et al. Acquired resistance of EGFR
-mutant lung cancer to a T790Mspecific EGFR inhibitor: Emergence of a third mutation (C797S) in the EGFR tyrosine kinase domain[ J ]. JAMA Oncol, 2015, 1( 7 ): 982 - 984.
[ 12 ]     张星贤，孙莉琼，戚    进. 酪氨酸激酶抑制剂类小分子抗肿瘤药物的研究进展[ J ]. Chinese Journaf of New D rugs，2018，27（ 22 ）：2 616 - 2 629.
[ 13 ]     Pawar V G, Sos M L, Rode H B, et al. Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor[ J ]. J Med Chem, 2010（ 53 ）: 2 892 - 2 901.
[ 14 ]     Carmi C, Cavazzoni A, Vezzosi S, et al.Novel irreversible epiderm-
al growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion[ J ]. J Med Chem, 2010（ 53 ）: 2 038 - 2 050.
[ 15 ]     薛子溪，陈国术. 含喹唑啉-芳基哌嗪结构新型抗肿瘤药物的设计合成[ J ]. 化学工程与装备，2017（ 5 ）：10 - 11.
[ 16 ]     孟祥川，栗    娜，李二冬，等. 2-甲硫基-4-芳胺喹唑啉衍生物的合成及抗肿瘤活性评价[ J ]. Chin J Org Chem, 2018（ 38 ）：3 063 - 3 069.