CAJ | 학술논문

甾体类药物由于其特有的生理活性而被广泛应用于各种疾病的治疗。本文采用鹅脱氧胆酸为原料,通过Jones试剂氧化其3,7-位的羟基,然后进一步与不同的芳杂环氨反应,进一步还原羰基,合成了6个新的具有不同结构特征的甾体芳杂环酰胺衍生物,合成物经IR、NMR及HRMS进行结构表征。同时采用人胃癌细胞(SGC-7901)和肝癌细胞(Bel-7404)对合成物进行了体外抑制肿瘤细胞生长增殖活性测试,结果表明其中的3,7-二羟基鹅脱氧胆酸芳杂环酰胺衍生物对所测试肿瘤细胞株具有明显的抑制活性。
치체류약물유우기특유적생리활성이피엄범응용우각충질병적치료。본문채용아탈양담산위원료,통과Jones시제양화기3,7-위적간기,연후진일보여불동적방잡배안반응,진일보환원탄기,합성료6개신적구유불동결구특정적치체방잡배선알연생물,합성물경IR、NMR급HRMS진행결구표정。동시채용인위암세포(SGC-7901)화간암세포(Bel-7404)대합성물진행료체외억제종류세포생장증식활성측시,결과표명기중적3,7-이간기아탈양담산방잡배선알연생물대소측시종류세포주구유명현적억제활성。
The steroidal drugs were widely applied in the cure of various diseases because of their special bioactivity. Using che-nodeoxycholic acid as starting material,some aromatic heterocycle chenodeoxycholate amides were synthesized by the oxidation with Jones,reacted with various aromatic amines and reduction by NaBH4. The structures of all compounds were characterized by IR, NMR and HRMS. The antiproliferative activity of the compounds was evaluated against human gastric cancer ( SGC-7901 ) and hu-man liver cancer(Bel-7404)cells. The results showed that some aromatic heterocycle chenodeoxycholate amide with 3,7-dihydroxyl groups exhibited distinct inhibitory activity to these cancer cells.