Recently, we have synthesized certain coumarin a-methylene-y-butyrolactorones for biological evaluations. Some of them were found to possess cardiovascular effects while others have been proved to be potential antiproliferative agents. A numbeier of oxime- and amide bearing quinolin-2(lH)-one derivatives have also been synthesized and demonstrated to possess anti-inflammatory and antiproliferative activities.To explore novel type of biologically active coumarin derivatives, we have synthesized a series of oxime and amide bearing coumarins and evaluated for their biological activities. These compounds were synthesized via alkylation of hydroxyylated coumarin precursors followed by the reaction with NH2OH or NaN3 (Schmidt reaction). The preliminary assays indicated that oxime-containing coumarin derivatives possessed good inhibitory activities on the fMLP-induced inflammation while the amide-conntaiaining coumarin derivatives exhibited potent antiproliferative activities against the growth of NPC-TW01, H661 and Jurkat cell lines. The cell cycle analysis showed that the amide-containing coumarin derivatives rested NPC-TW01 cells at S phase with dose-dependent manner.
