Synthesis and cytotoxicity of 3,4-diaryl-2(5H)-furanones

A series of 3,4-diaryl-2(5H)-furanone derivatives were synthesized and evaluated for their cytotoxicity in a small panel of cancer cell lines. Four out of 10 compounds in this series, for example 3-(3,4,5-trimethoxyphenyl)-4-(4-methoxyphenyl)-, 3-(3,4,5-trimethoxyphenyl)-4-(3-hydroxy-4-methoxyphenyl)-, 3- (3,4,5-trimethoxyphenyl)-4-(3-amino-4-methoxyphenyl)-, and 3-(3,4,5-trimethoxyphenyl) -4- (2-naphthyl)-2(5H)-furanones, were found to have potent cytotoxic activities with ED50 values of less than 20 nM in most of the cell lines tested. (C) 2002 Elsevier Science Ltd. All rights reserved.