目的设计合成2,5-二亚苄基环戊酮类化合物,并对其抗肿瘤活性进行初步的评价。方法以环戊酮为起始原料,通过Stork烯胺反应、Aldol缩合、Mannich反应制备目标化合物;并采用MTT法测试目标化合物对人慢性粒细胞白血病急变细胞株K562增殖的抑制活性。结果与结论共合成了15个未见文献报道的2,5-二亚苄基环戊酮Mannich碱类化合物,其结构经1H-NMR和MS确证。初步药理结果显示9个目标化合物对K562的增殖抑制作用强于姜黄素。
A series of novel monocarbonyl curcumin derivatives was designed for enhanced stability and im- proved water-solubility. Fifteen novel 2,5-bisbenzylidenecyclopentanone derivatives bearing hydrophilic ami- no moiety were synthesized from cyclopentanone and arylaldehydes via Stork reaction, Aldol condensation and Mannich reaction, and characterized by 1H-NMR and MS spectra. The antiproliferative effects of the tar- get compounds against CML K562 cells were evaluated by MTT assay. Preliminary pharmacologicals results showed that nine compounds were more potent than curcumin. The structure-activity relationships revealed that the introduction of piperazinyl moiety was of benefit to the enhanced antiproliferative activity.