靛红杂合喹唑啉类化合物的合成及抗肿瘤活性研究

发布时间：2018-04-15 13:46

本文选题：靛红 + 喹唑啉　；参考：《有机化学》2017年07期

【摘要】：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.
[Abstract]:Nine quinazoline target compounds with indirubin heterozygotes were synthesized. The structures of the target compounds were characterized by NMR-IR and HRMS. The structure of the target compounds was further determined by crystal culture and X-ray diffraction data.At the same time, the antitumor activity of these compounds was evaluated in vitro on human colorectal cancer cell line SW480, human non-small cell lung cancer cell line A549 and NCI-H1975and human epidermal squamous carcinoma cell A431 by thiazolyl blue MTT assay.The results showed that most of the target compounds could inhibit the proliferation of tumor cells.In particular, the compounds of Ela-3-Hypo (Elae) 5-Na-4 (acetylaniline) quinazoline (6-yl) furan (-2-yl) methylene))) indolinoline (2-one) 4aanine showed a good inhibitory effect on the proliferation of tumor cells in the four kinds of tested tumor cells, and the results showed that the inhibition of the proliferation of the tumor cells was obvious in the four kinds of tumor cells, and the inhibitory effect of the compounds on the proliferation of the tumor cells was also observed.Its effect is superior to that of Rabatini, an anti-tumor drug used in clinic.
【作者单位】：陕西师范大学化学化工学院教育部药用资源与天然药物化学重点实验室;
【基金】：国家自然科学基金(No.21272144)资助项目~~
【分类号】：O626;R914;R96

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