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A series of new 2-propylpyrido[2,3-d]pyrimidin-4(3H)-one with different substituents at position 3 were synthesized by traditional method and Iodine catalyst method. The effect of the newly synthesized compounds was tested as anti-cancer in National Cancer Institute(NCI)in USA. Some of the synthesized compounds exploited potent antitumor activity, especially the compounds pyrido[2,3-d][1,3]oxazin (2), 3-amino derivative 3a, 3b and hydroxy derivative 3c displayed the highest activity among thedoi:10.11648/j.sjc.20130101.11 fatcat:5gnqnu7bxvf3pp5lnpwtk5xjme