A　series　of　1,4-bis(2,3-dihydro-5-oxopyrrol-4-yl)-1,3-butadienes　were　designed　as　inhibitors　of　checkpoint　kinase　1　(Chk1),　based　on　the　structureaEuro＇activity　relationships　for　known　inhibitors　through　docking　simulations.　The　docking　results　suggested　that　the　title　compounds　were　similar　to　known　inhibitors　in　interaction　with　the　catalytic　site　of　Chk1.　Twelve　compounds　were　synthesized　by　a　one-pot　procedure　from　amines,　dimethyl　acetylenedicarboxylate,　and　glyoxal　in　water　in　the　presence　of　catalytic　amounts　of　gamma-cyclodextrin.　The　inhibitory　activities　of　the　synthesized　compounds　were　evaluated　in　vitro　using　EC9706　esophageal　cancer　cells.　The　results　indicated　that　1,4-bis(2,3-dihydro-5-oxopyrrol-4-yl)-1,3-butadienes　significantly　inhibited　Chk1　(IC50　10.45　mu　M).