| 韦娇梅,余佳,余刚,曾晓萍,徐广灿,徐必学.化学通报,2022,85(6):709-716. |
| 新型含三氟甲基喹唑啉衍生物的设计合成及抗肿瘤活性研究 |
| Design, Synthesis and Antitumor Activity of Novel Trifluoromethylquinazoline Derivatives |
| 投稿时间：2021-11-19 修订日期：2021-12-20 |
| DOI： |
| 中文关键词: 喹唑啉 三氟甲基 合成 抗肿瘤活性 |
| 英文关键词:quinazoline trifluoromethyl synthesis antitumor activity |
| 基金项目:贵州省高层次创新型人才培养计划（黔科云平台人才［2016］5678） |
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| 中文摘要: |
| 为了从喹唑啉衍生物中寻找高活性的抗肿瘤分子，以2-氨基苯甲酰胺为原料，经过三氟乙酰化、环化、氯代、以及偶联反应等，设计合成了21个2-三氟甲基喹唑啉类化合物，并通过1H NMR、13C NMR、19F NMR进行结构确证；采用四唑盐（MTT）法评价目标化合物的体外抗肿瘤活性。结果表明，多数喹唑啉衍生物对人前列腺癌细胞（PC3、LNCaP）、人慢性髓系白血病细胞（K562）、宫颈癌细胞（Hela）以及人肺癌细胞（A549）具有抗增殖活性，其中活性较好的化合物5a和5b在5 μmol·L-1时对LNCaP细胞增殖的抑制活性分别为53.4%、55.2%，其活性与紫杉醇相当。此外N-甲基化产物5a和5b的体外抗肿瘤活性较原型化合物（4a和4b）显著提高，这为该类化合物的深入研究提供参考依据。 |
| 英文摘要: |
| In order to find efficient anti-tumor target compounds in quinazoline derivatives, a series of 2-trifluoromethylquinazoline derivatives were synthesized by trifluoacylation, cyclization, chlorination and coupling reaction. Their chemical structures were characterized by 1H NMR, 13C NMR, 19F NMR and their anti-tumor activities in vitro were demonstrated by MTT assay method. The results showed that most of synthesized quinazoline derivatives showed inhibitory effect on human prostate cancer cells (PC3 and LNCaP), chronic myelogenous leukemia (K562), cervical cancer cells (Hela) and human lung cancer cells (A549), among them, compounds 5a and 5b with better activities against LNCaP at 5 μmol·L-1 were 53.4% and 55.2%, respectively. Its activity was equivalent to taxol. In addition, the in vitro anti-tumor activities of the N-methylated products 5a and 5b were significantly higher than the corresponding prototype compounds (4a and 4b) which provide a basis for further research of the 2-trifluoromethylquinazoline derivatives. |
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