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合成了9种靛红杂合的喹唑啉类目标化合物,借助NMR、IR和HRMS对目标化合物进行了结构表征,并通过晶体的培养及X射线衍射数据进一步确定了目标化合物的结构.同时采用噻唑蓝(MTT)法在人结直肠癌细胞SW480、人非小细胞肺癌细胞A549和NCI-H1975、人表皮鳞癌细胞A431上对这些化合物进行了抗肿瘤活性的初步体外评价.结果表明,大部分目标化合物具有明显的抑制肿瘤细胞增殖的作用,尤其是化合物(E)-3-(((E)-(5-(4-(3-乙炔苯胺基)喹唑啉-6-基)呋喃-2-基)亚甲基)亚肼基)吲哚啉-2-酮(4a),在4种所试肿瘤细胞上均表现出良好的抑制肿瘤细胞增殖的作用,其效果优于临床使用的抗肿瘤药物拉帕替尼.
Nine target isomers of quinazolines were synthesized, and the target compounds were characterized by means of NMR, IR and HRMS. The structures of target compounds were further confirmed by crystal growth and X-ray diffraction data. MTT assay was used to evaluate the anti-tumor activity of these compounds in human colorectal cancer cells SW480, human non-small cell lung cancer cells A549 and NCI-H1975, and human epidermoid squamous cell carcinoma A431 cells.The results showed that large Some of the target compounds have obvious inhibitory effect on the proliferation of tumor cells, especially the compounds (E) -3 - ((E) - (5- (4- (3-ethynylanilino) quinazolin- Yl) methylene) hydrazono) indolin-2-one (4a) showed a good effect of inhibiting the proliferation of tumor cells on the 4 kinds of tested tumor cells, and the effect was superior to that of clinical use The antitumor drug lapatinib.