[关键词]
[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。
[Key word]
[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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[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)