高等学校化学学报2023，Vol.44Issue(12)：61-70,10.DOI:10.7503/cjcu20230337
含香豆素结构的1,4-戊二烯-3-酮类衍生物的合成及生物活性
Synthesis and Bioactivities of Penta-1,4-dien-3-one Derivatives Containing a Coumarin Moiety
摘要
Abstract
Aiming to develop novel candidates for antitumor drugs,sixteen monocarbonyl curcumin derivatives were constructed by dexterously intergrating a coumarin fragment into the penta-1,4-dien-3-one skeleton deriving from the structural optimization of a curcumin molecule.After structural confirmations,the above derivatives were tested by a methyl thiazolyl tetrazolium(MTT)colorimetric assay for their inhibitory activities against the in vitro proliferation of gastric cancer cells(SGC7901)and hepatoma carcinoma cells(HepG2).The bioassay results demonstrated that most of synthesized molecules exhibited outstanding inhibitory effects against the in vitro proliferation of SGC7901 and HepG2 cells.Strikingly,the half maximal inhibitory concentrations(IC50)of compounds 4c and 4j against SGC7901 cells reached 0.22 and 0.27 µmol/L,respectively,which are obviously better than that of epirubicin(1.23 µmol/L).Meanwhile,the IC50 value of compounds 4l against HepG2 cells reached 0.47 µmol/L that is observably superior to that of epirubicin(2.30 µmol/L).Subsequently,morphological observations reconfirmed the outstanding advantage of coumarin-containing penta-1,4-dien-3-ones on inhibiting the in vitro proliferation of tumor cells,which implied these distinctive derivatives could be further developed as novel candidates for antitumor drugs.关键词
1,4-戊二烯-3-酮/香豆素/先导发现与优化/抗肿瘤活性Key words
Penta-1,4-dien-3-one/Coumarin/Lead discovery and optimization/Antitumor activity分类
化学化工引用本文复制引用
王晓斌,王瑞颖,董雪,严莉莉,张娟,顾一飞,程青芳,薛伟..含香豆素结构的1,4-戊二烯-3-酮类衍生物的合成及生物活性[J].高等学校化学学报,2023,44(12):61-70,10.基金项目
国家自然科学基金(批准号:32202334)、江苏省高等学校自然科学基金(批准号:22KJB210009)、江苏海洋大学人才引进项目(批准号:KQ21031)和江苏海洋大学研究生科研与实践创新计划项目(批准号:KYCX202340)资助.Supported by the National Natural Foundation of China(No.32202334),the Natural Science Foundation of Jiangsu University,China(No.22KJB210009),the Research Fund for Talent Introduction of Jiangsu Ocean University,China(No.KQ21031)and the Postgraduate Research&Practice Innovation Program of Jiangsu Ocean University,China(No.KYCX202340). （批准号:32202334）
