首页|新型2-氨基-4-苯基-3-氰基-4H-吡喃并熊果酸衍生物的设计合成及活性研究

新型2-氨基-4-苯基-3-氰基-4H-吡喃并熊果酸衍生物的设计合成及活性研究

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以熊果酸为原料,经过氧化、缩合、取代、环化四步反应得到2-氨基-4-苯基-3-氰基-4H-吡喃并熊果酸衍生物4a、4b和4c,其结构经过1H NMR、13C NMR、HRMS确证.采用CCK-8法评价化合物4a～4c对人非小细胞肺癌细胞株(A549)、人肺腺癌耐顺铂细胞株(A549/DDP)的抗增殖活性,化合物4a～4c对A549及A549/DDP细胞的抑制活性都优于阳性对照药物顺铂,其中化合物4b对A549/DDP细胞表现出良好的体外抑制活性[IC50=(0.087±0.003)μmol/L]及选择性.
Design,Synthesis and Antitumor Evaluation of 2-Amino-4-phenyl-3-cyano-4H-pyran-ursolic Acid Hybrids
Using ursolic acid as the raw material,2-amino-4-phenyl-3-cyano-4H-pyran-ursolic acid hybrids of 4a,4b,and 4c were synthesized through four steps of reactions:oxidation,condensation,substitution,and cyclization.Their structures were characterized by 1H NMR,13C NMR and HRMS.The antiproliferative activities of compounds 4a to 4c against human non-small cell lung cancer cells(A549)and cisplatin-resistant human lung adenocarcinoma cells(A549/DDP)were evaluated using the cell counting kit-8(CCK-8).Compounds 4a to 4c exhibited superior inhibitory activities against both A549 and A549/DDP cells compared to the positive control drug cisplatin.Among them,compound 4b demonstrated notable in vitro antiproliferative activity[IC50=(0.087±0.003)μmol/L]and selectivity towards A549/DDP cells.

ursolic acid2-amino-4-phenyl-3-cyano-4H-pyranchromenescisplatin-resistant human lung adenocarcinoma cells

杨俊、黄蕊、杨显娟、舒海霞、梁光平

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遵义医药高等专科学校,贵州遵义 563006

熊果酸 2-氨基-4-苯基-3-氰基-4H-吡喃 色烯 人肺腺癌耐顺铂细胞株A549/DDP

遵义市科技合作计划项目遵义市科技合作计划项目贵州省第六批高层次创新型人才遴选培养计划——千层次人才项目

遵市科合HZ字2023459号2023454号黔委人领办发[2022]3号

2024

10.19342/j.cnki.issn.1009-9212.2024.05.003

精细化工中间体
湖南化工研究院

精细化工中间体

CSTPCD
影响因子：0.236
ISSN：1009-9212
年,卷(期)：2024.54(5)