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Nine 5-aryl-2-methyloxazole derivatives were synthesized via gold-catalyzed alkyne oxidation.All of the compounds have been screened for their antiproliferative activities against MCF-7 cell(human breast carcinoma),A549 cell(human lung carcinoma)and Hela cell(human cervical carcinoma)lines in vitro.The results revealed that compounds 1b,1c and 1d exhibited strong inhibitory activities against the MCF-7 cell lines(with IC50values of 4.6,9.7 and 2.2 mmol/L,respectively).