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The starting 1-phenylbutane-1,3-dione (1) was used as key intermediate for the synthesis of several new thiophene and pyrazole derivatives. The newly synthesized compounds were evaluated for in vitro cytotoxicity against an Ehrlich ascites cells and in vivo cytotoxicity for compound 10d using EAC assay and 5-fluorouracil is used as reference drug. Compounds 7c, e and 10c, d showed significant activity in certain cancer cell and have been targeted for further studies, compound 10d is moredoi:10.4236/pp.2012.32022 fatcat:qia2lfqdlvgltknlu5n5qad6bu