烷氧基联苯/姜黄素偶联物的合成及抗耐药肿瘤活性

摘要

Objecti ve To design and synthesize conjugates of alkoxylbiphenyl/C5-curcumine with antitumor activities. Methods Bicyclol,acetone and benzaldehyde with various substituents were used as raw materials. The target compounds were obtained by oxidizing and Aldol condensation reaction. And their antitumor activities were evaluated by MTS assay in the parental sensitive K562 and drug-resistant K562/A02 cell lines. Results Twelve alkoxylbiphenyl/C5-curcumine conjugates were prepared. Conclusion The synthetic procedure of the target compounds is simple,and the yield is high. Compound 3b could significantly inhibit K562 and drug-resistant K562/A02 cell proliferation,and the IC50 is 5.38 and 3.60μmol/L,respectively.%目的设计、合成具有抗肿瘤活性的烷氧基联苯/C5-姜黄素偶联物。方法以双环醇、丙酮及不同取代的苯甲醛为原料，经吡啶氯铬酸盐（pyridinium chlorochromate，PCC）氧化、两步Aldol缩合反应制备目标化合物。采用MTS法评价目标化合物对敏感K562及耐药K562/A02细胞的增殖抑制作用。结果制备了12个烷氧基联苯/C5-姜黄素偶联物。结论该类化合物的合成路线简单、收率高。化合物3b对敏感及耐药K562细胞均具有显著的增殖抑制作用，其IC50分别为5.38和3.60μmol/L。