异海松酸基杂环酰胺衍生物的制备及抗癌活性
Preparation and anticancer activity of isopimaric acid heterocyclic amide derivatives
刘娟娟 1张珺 1杨韶平1
作者信息
- 1. 贵州中医药大学 药学院,贵州 贵阳 550025
- 折叠
摘要
为了获得结构新颖的抗肿瘤药物分子,以天然产物异海松酸(Ⅰ)为母体结构,合成了 9 个异海松酸基杂环酰胺化合物(Ⅱa～Ⅱi),其结构经FTIR、1HNMR、13CNMR和TOF-MS确证.抗肿瘤活性测试结果表明,除Ⅱf 外,其余目标化合物的抗肿瘤活性均比母体化合物异海松酸的活性高,尤其是含有吡嗪杂环的化合物异海松酸基(2-氨基吡嗪)酰胺(Ⅱd)对人黑色素瘤(A375)细胞显示出显著的增殖抑制活性,其半抑制浓度(IC50)为 13.34 μmol/L,有望通过进一步结构修饰来提高活性,成为异海松酸类抗癌先导化合物.
Abstract
In order to develop antitumor drugs with new molecular structure,nine heterocyclic amide compounds(Ⅱa～Ⅱi)were synthesized from natural product isopimaric acid(Ⅰ),and characterized by FTIR,1HNMR,13CNMR and TOF-MS.Data from anti-tumor performance analysis revealed that except forⅡf,all the other target compounds showed higher anti-tumor activities than the natural isopimaric acid.Especially compound isopimaric acyl-(2-aminopyrazine)amide(Ⅱd)containing pyrazine heterocycle exhibited significant cell proliferation inhibitory activity against A375 human melanoma cells,with a half maximal inhibitory concentration(IC50)of 13.34 μmol/L.Therefore,compound Ⅱd is expected for antitumor activity improvement through further structural modification and become a leading anti-tumor compound of isopimaric acid.
关键词
异海松酸/杂环化合物/合成/抗癌活性/增殖抑制/医药原料Key words
isopimaric acid/heterocyclic compounds/synthesis/anticancer activity/proliferation inhibition/drug materials引用本文复制引用
出版年
2024
NETL
NSTL
万方数据