新型喹唑啉类衍生物的合成与抗肿瘤活性的研究
The synthesis and anti-tumor activity research of a novel quinazoline derivatives
作者：邵薇;何谷;成丽;
Author：
收稿日期： 年卷（期）页码：2013,28(03):-232-234
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：喹唑啉类衍生物;表皮生长因子抑制剂;合成;抗肿瘤活性
Key words：
基金项目：国家自然科学基金资助项目(批准号:81001357)
中文摘要
目的合成一类新型的喹唑啉类衍生物并研究其体外抗肿瘤活性。方法以2-氨基-5-硝基苯甲腈为起始原料,经过环合、氯化、氨基取代、硝基还原、N-乙酰化等反应得到目标化合物,采用MTT法在前列腺癌细胞PC-3、人卵巢癌细胞SKOV-3、人结直肠癌细胞HCT116、皮肤基底细胞癌细胞A431和人红白血病细胞K562等细胞株上进行了体外抗肿瘤活性测试。结果和结论合成了3个新型化合物,并经1HNMR、MS确证了化学结构。初步的体外抗肿瘤活性显示化合物具有抗白血病和抗结肠癌活性。
参考文献
[1]Herbst RS.Review of epidermal growth factor receptor biology[J].Int J Radiat Oncol Biol Phy,2004,59:21-26.
[2]Yosef Y,Joseph S.Epidermal growth-factor induces rapid,rever-sible aggregation of the purified epidermal growth-factorreceptor[J].Biochemistry,2004,26(5):1443-1451.
[3]Barker AJ,Gibson KH,Grundy W,et al.Studies leading to theidentification of ZD 1839(Iressa):A norally active,selectiveepider-malgrowth factor receptor tyrosine kinase inhibitor targe-ted to the treatment of cancer[J].Bioorg Med Chem Lett,2001,11:1911-1914.
[4]Stefan T,Tanja W,Rolf K,et al.Substituted 2-arylbenzothia-zoles as kinase inhibitors:Hit-to-lead optimization[J].BioorgMed Chem,2009,17:6728-6737.
[5]Kwak EL,Sordella R,Bell DW,et al.Irreversible inhibitors of theEGF receptor may circumvent acquired resistance to gefitinib[J].Proc Natl Acad Sci USA,2005,102:7665-7670.
[6]Juozas D,Fabienne D,Bertrand JJC,et al.The combi-targetingconcep:Synthesis of stable nitrosoureas designed to inhibit theepidermal growth factor receptor(EGFR)[J].J Med Chem,2006,49:3544-3552.
[7]陆涛,焦宇,陈亚东,等.Raf激酶抑制剂及其制备方法和用途[P].200710022 0504.2008-09-10.
【关闭】
