A series of curcumin analogues including new 4-arylidene curcumin analogs (4-arylidene-1,7-bisaryl-hepta-1,6-diene-3,5-diones) were synthesized. Cell growth inhibition assays revealed that most 4-arylidene curcumin analogs can effectively decrease the growth of a panel of lung cancer cells in sub- and low micromolar concentration ranges. High content analysis technology coupled with biochemical studies showed that this new class of 4-arylidene curcumin analogs exhibits significantly improved NF-κB inhibition activity over the parent compound curcumin, at least in part by inhibiting IκB phosphorylation and degradation via IKK blockage; selected 4-arylidene curcumin analogs also reduced the tumorigenic potential of cancer cells in a clonogenic assay.

An efficient one‐pot synthesis of multi‐functionalized chromeno[2,3‐c]pyrrol‐9(2H)‐ones from 1,3‐diaryl‐1,3‐diketones and amino acids is described. The synthesis is based on the 4‐(dimethylamino)pyridine‐catalyzed Baker–Venkataraman rearrangement and subsequent reactions.

No abstract

No abstract