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[1] 何谷[2] 成丽[1] 

机构地区：[1]四川大学华西药学院,四川成都610041 [2]四川大学生物治疗国家重点实验室,四川成都610041

出　　处：《华西药学杂志》2013年第3期232-234,共3页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:81001357)

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。OBJECTIVE To synthesize a novel quinazoline derivatives and study their antitumor activity in vitro.METHODS The target compounds were synthesized from 5-nitroanthranilonitrile by cyclization,halogenation,amino substitution,nitro reduction,N-acylation etc..The anti-tumor activity in vitro of these compounds have been studied by MTT assay with prostate carcinoma PC-3 cells,ovarian carcinoma SKOV-3 cells,human colorectal cancer HCT116 cells,human epithelial carcinoma A431 cells and human erythroleukemia K562 cells.RESULTS and CONCLUSION Three new compounds were synthesized,and the chemical structures were characterized by 1HNMR and MS.Preliminary anti-tumor activity in vitro showed that compound Ⅵa has a good anti-erythroleukemia and anti-colorectal carcinoma activity.

关 键 词：喹唑啉类衍生物 表皮生长因子抑制剂 合成 抗肿瘤活性 

分 类 号：R914[医药卫生—药物化学]