辽宁大学学报（自然科学版）2026，Vol.53Issue(1)：62-71,10.
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
Synthesis and Anticancer Activity of Thieno[3,2-d]pyrimidine Derivatives Bearing Piperidylcarboxamide Moiety
摘要
Abstract
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).关键词
噻吩并[3,2-d]嘧啶/合成/抗肿瘤活性/MTT法Key words
thieno[3,2-d]pyrimidine/synthesis/anticancer activity/MTT assays分类
医药卫生引用本文复制引用
刘举,林艺涵,吴霜,丁实,张志成,韩恩惠,陈烨,沈继伟..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[J].辽宁大学学报（自然科学版）,2026,53(1):62-71,10.基金项目
沈阳市自然科学基金(23-503-6-12) （23-503-6-12）
辽宁省自然科学基金计划项目面上项目(2022-MS-169) （2022-MS-169）
