| 4-苯基-1,3,5-三嗪-2-胺类衍生物的合成及其体外抗肿瘤活性研究 |
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| 引用本文： | 李唯,郭舜民,陈阿虹,阙慧卿,林绥.4-苯基-1,3,5-三嗪-2-胺类衍生物的合成及其体外抗肿瘤活性研究[J].现代药物与临床,2019,34(8):2253-2257. |
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| 作者姓名： | 李唯 郭舜民 陈阿虹 阙慧卿 林绥 |
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| 作者单位： | 福建省医学科学研究院 福建省医学测试重点实验室,福建 福州,350001;福建省医学科学研究院 福建省医学测试重点实验室,福建 福州,350001;福建省医学科学研究院 福建省医学测试重点实验室,福建 福州,350001;福建省医学科学研究院 福建省医学测试重点实验室,福建 福州,350001;福建省医学科学研究院 福建省医学测试重点实验室,福建 福州,350001 |
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| 基金项目： | 福建省自然科学基金资助项目（2017J01141）；福建省省属公益类科研院所基本科研专项（2015R1031-1），福建省医学创新项目（2017-CX-12） |
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| 摘 要： | 目的以IMC-038525为先导化合物,设计并合成4-苯基-1,3,5-三嗪-2-胺类化合物,考察其体外抗肿瘤活性。方法以2,4-二氯-1,3,5-三嗪为起始原料,经过氨化、Suzuki偶联和还原胺化合成一类4-苯基-1,3,5-三嗪-2-胺类化合物,采用噻唑蓝法(MTT)测定其对肿瘤细胞的抑制活性。结果设计并合成了13个新化合物,结构经1H-NMR和MS确证。活性测试结果显示该类化合物具有一定的抗肿瘤活性。结论合成了一类4-苯基-1,3,5-三嗪-2-胺类衍生物,具有一定抑瘤活性的化合物,为新型抗肿瘤化合物的设计与合成提供思路。
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| 关 键 词： | IMC-038525 抗肿瘤化合物 血管靶向药物 |
| 收稿时间： | 2019/3/5 0:00:00 |
Synthesis of 4-phenyl-1,3,5-triazine-2-amine derivatives and their antitumor activities in vitro |
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| LI Wei,GUO Shun-min,CHEN A-hong,QUE Hui-qing and LIN Sui.Synthesis of 4-phenyl-1,3,5-triazine-2-amine derivatives and their antitumor activities in vitro[J].Drugs & Clinic,2019,34(8):2253-2257. |
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| Authors: | LI Wei GUO Shun-min CHEN A-hong QUE Hui-qing and LIN Sui |
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| Institution: | Fujian Provincial Key Laboratory of Medical Analysis, Fujian Academy of Medical Sciences, Fuzhou 350001, China,Fujian Provincial Key Laboratory of Medical Analysis, Fujian Academy of Medical Sciences, Fuzhou 350001, China,Fujian Provincial Key Laboratory of Medical Analysis, Fujian Academy of Medical Sciences, Fuzhou 350001, China,Fujian Provincial Key Laboratory of Medical Analysis, Fujian Academy of Medical Sciences, Fuzhou 350001, China and Fujian Provincial Key Laboratory of Medical Analysis, Fujian Academy of Medical Sciences, Fuzhou 350001, China |
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| Abstract: | Objective To synthesize 4-phenyl-1,3,5-triazine-2-amine derivatives and evaluate their antitumor activities, according to the skeleton transition of the lead compound IMC-038525. Methods 2,4-Dichloro-1,3,5-triazine was used as starting materials to synthesize a series of 4-phenyl-1,3,5-triazine-2-amine derivatives through amination, Suzuki couple reaction, and reductive amination. The inhibitory activity of tumor cells was determined by methyl thiazolyl tetrazoliym (MTT) assay. Results Thirteen target compounds were synthesized in the article, and their chemical structures were confirmed by MS and 1HNMR. Antitumor activities test showed some target compounds had antitumor activities. Conclusion A series of 4-phenyl-1,3,5-triazine-2-amine derivatives are synthesized with some antitumor activities, which offer new mentality to designe and synthesize novel antitumor compounds in the future. |
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| Keywords: | IMC-038525 antitumor agent vascular targeting drug |
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