[摘要]：A series of ethyl 3-aryl-4-oxo-3,3a,4,6-tetrahydro-1H-furo[3,4-c]pyran-3a-carboxylates were prepared through the metal-catalyzed domino reaction of alkylidene malonates and 1,4-butynediol under a one-pot reaction condition at room temperature. Their in vitro anti-proliferative activities were subsequently evaluated in A549, QGY and HeLa cells. The majority of the compounds showed potent anti-tumor activity against HeLa cells. In particular, compound 31 was the most potent compound with IC50 value of 5.4 mu M. For the first time, the X-ray structure of the anti-tumor ethyl 3-aryl-4-oxo-3,3a, 4,6-tetrahydro-1H-furo[3,4-c]pyran-3a-carboxylates is determined. (C) 2011 Elsevier Ltd. All rights reserved.
