A series of 4,5-diarylisoxazoles related to combretastatin A-4 (CA-4) were synthesized and evaluated for cytotoxicity against three human cancer cell lines. Among them, compound 6e showed better cytotoxic activity than CA-4 in HeLa and HepG2 cell lines assayed with IC50 value as low as 0.022 and 0.065 nM, respectively. (c) 2006 Elsevier Ltd. All rights reserved