新型喹唑啉类衍生物的合成与初步抗肿瘤活性的研究
Synthesis and preminlinary anti-tumor activities of novel quinazoline derivatives
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、氯化反应、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VIa具有良好的抗白血病和抗结肠癌活性。
OBJECTIVE To synthesize a novel of quinazoline derivatives and study their antitumor activity in vitro. METHODS The target compounds were synthesized from 5-nitroanthranilonitrile by cyclization, halogenation, amino substituted，nitro reduction，N-acylation etc.. The anti-tumor activity in vitro of these compounds have been studied 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, using MTT assay. RESULTS and CONCLUSION Three new compounds were prepared, and the chemical structures were characterized by 1HNMR and MS. Preliminary anti-tumor activity in vitro displays that compound VIa has a good anti- erythroleukemia and anti-colorectal carcinoma activity.
何谷、成丽、邵薇
肿瘤学药学基础医学
药物化学喹唑啉类衍生物表皮生长因子抑制剂合成，
Medicinal Chemistryquinazoline derivativesEGFR inhibitorssynthesis
何谷,成丽,邵薇.新型喹唑啉类衍生物的合成与初步抗肿瘤活性的研究[EB/OL].(2012-12-28)[2025-05-18].http://www.paper.edu.cn/releasepaper/content/201212-1180.点此复制
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