鹰嘴豆芽素色烯类拼接衍生物的合成及其抗白血病活性

Synthesis and Anti-human Leukemia Cells Activities of Chromene-biochanin Hybrids

以鹰嘴豆芽素与丙二腈芳基烯烃(2),在催化剂Ca(OH)_(2)催化下,在甲醇回流下发生Michael加成环化反应,获得合成了9个新颖的鹰嘴豆芽素色烯类拼接衍生物3a~3i,产率78%~85%,其结构经^(1)H NMR,^(13)C NMR和HR-MS(ESI-TOF)表征。采用MTT法研究了3a~3i对人白血病细胞(K562)的体外抗肿瘤活性。结果表明:化合物3a~3d对K562具有一定的抑制活性,说明鹰嘴豆芽素色烯类骨架可以作为先导化合物,进行进一步的研究。

Nine new chromene-biochanin hybrids(3a~3i)were synthesized via a Ca(OH)_(2)-catalyzed Michael addition and then cyclization reaction of biochanin with arylidenemalononitriles(2)under reflux conditions in MeOH for 8 h.The yields of 3a~3i were 78%-85%.The structures of products were characterized by ^(1)H NMR,^(13)C NMR and HR-MS(ESI-TOF).The in vitro antitumor activities against human leukemia cells(K562)were demonstrated by MTT assays using the commercially available broad-spectrum anticancer drug Cisplatin as a positive control.The results showed that compounds 3a~3d showed good cytotoxic effects,which suggested that chromene-biochanin hybrids may be potential leads for further biological screenings.