含哌啶酰胺结构的噻吩并[3,2-d]嘧啶衍生物合成与抗肿瘤活性OA
Synthesis and Anticancer Activity of Thieno[3,2-d]pyrimidine Derivatives Bearing Piperidylcarboxamide Moiety
为得到新型抗肿瘤化合物,设计并合成了17 个含哌啶酰胺结构的噻吩并[3,2-d]嘧啶类化合物,并对该类化合物的体外肿瘤活性进行了初步研究.目标化合物的结构通过氢核磁共振波谱(1 H NMR)、高分辨碳核磁共振波谱(13 C NMR)和电喷雾电离质谱(HRMS(ESI))表征.采用3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐比色法(MTT法)评价了目标化合物体外对人肺腺癌细胞株A549 和人肝癌细胞株HepG2 的抗肿瘤活性.实验结果表明,17 个化合物对两种肿瘤细胞株均具有很好的抑制活性.其中,化合物Ⅵk活性突出,对A549 和HepG2 两种肿瘤细胞株的半数抑制浓度IC50值分别为2.46 μmol/L和4.37 μmol/L,与阳性对照药索拉非尼(IC50值分别为3.02 μmol/L和3.34 μmol/L)的活性相当.
To find novel antitumor agents,seventeen novel thieno[3,2-d]pyrimidine derivatives bearing piperidylcarboxamide moiety were successfully designed,synthesized and evaluated their anticancer activities.The structures of the target compounds were confirmed by 1 H nuclear magnetic presonance(1 H NMR),13 C nuclear magnetic resonance(13 C NMR)and high resolution mass spectrometry(HRMS)(eletrospray ionization,ESI).A549 and HepG2 cell lines were employed to evaluate anticancer activities of the target compounds using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay(MTT)-based assay in vitro.All the 17 newly synthesized compounds exhibited excellent antiproliferative activity against the tested two cell lines.Among them,compound Ⅵk showed outstanding inhibitory activity against A549 and HepG2 cell lines with IC50 value of 2.46 μmol/L and 4.37 μmol/L,respectively,which were comparable to the activity of the positive control drug sorafenib(3.02 μmol/L and 3.34 μmol/L).
刘举;林艺涵;吴霜;丁实;张志成;韩恩惠;陈烨;沈继伟
辽宁大学 药学院,辽宁 沈阳 110036辽宁大学 药学院,辽宁 沈阳 110036辽宁大学 药学院,辽宁 沈阳 110036辽宁大学 药学院,辽宁 沈阳 110036辽宁大学 药学院,辽宁 沈阳 110036辽宁大学 药学院,辽宁 沈阳 110036辽宁大学 药学院,辽宁 沈阳 110036辽宁大学 药学院,辽宁 沈阳 110036
医药卫生
噻吩并[3,2-d]嘧啶合成抗肿瘤活性MTT法
thieno[3,2-d]pyrimidinesynthesisanticancer activityMTT assays
《辽宁大学学报（自然科学版）》 2026 (1)
62-71,10
沈阳市自然科学基金(23-503-6-12)辽宁省自然科学基金计划项目面上项目(2022-MS-169)
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