摘要
以间苯二酚为原料,经过酰化、醚化反应合成了15个丹皮酚及其衍生物,以HeLa、MCF-7细胞为靶细胞,采用MTT法进行了初步的体外抗肿瘤活性研究。结果表明,4-位甲氧基是丹皮酚抗肿瘤活性的增效官能团,酮羰基侧链为丹皮酚抗肿瘤活性的必需官能团,与羰基相连侧链的碳原子数小于4时,随着侧链的延长其抗肿瘤细胞增殖活性会不断加强,优选出的化合物2d对HeLa和MCF-7细胞株具有较显著的抗增殖活性,IC50值分别为2.67和4.74μmol.L-1,这为丹皮酚抗肿瘤活性构效关系的研究打下了基础,值得进一步研究。
A series of paeonol derivatives have been synthesized by simple acylation and etherification of the paeonol. Anti-tumor activities of the synthesized compounds were evaluated against HeLa and MCF-7 cells lines in vitro by the standard MTT assay. It was found that the derivatives were more active against HeLa than MCF-7. The results also indicated that 4-methoxy group is the synergistic group ofpaeonol＇s anti-tumor activity and ketone carbonyl side chain is essential functional group of paeonol＇s anti-tumor activity. Compound 2d had stronger antiproliferative activities than paeonol against HeLa and MCF-7 cell lines with IC50 values of 2.67 and 4.74 μmol.L-1 respectively. The results showed that paeonol derivatives were worth to be intensively studied further.
出处
《药学学报》
CAS
CSCD
北大核心
2012年第1期72-76,共5页
Acta Pharmaceutica Sinica
基金
国家自然科学基金资助项目(20872118,30070905)
教育部博士点基金资助项目(20070697012)
陕西省重大科技专项资助项目(2008ZDKG-67)
陕西省重点实验室基金资助项目(08JZ74)
关键词
丹皮酚
衍生物
合成
抗肿瘤活性
paeonol
derivative
synthesis
anti-tumor activity
