A series of substituted chalcones and their corresponding pyrazoles were synthesized and evaluated for in vitro cytotoxic activity against a panel of human cancer cell lines. Out of 93 compounds screened, 8 compounds, 1s, 3i, j, n, 4i, j, n and 4s, showed marked activity. Compounds 4j, n and 4s were found to be the most promising in this study. SAR is also discussed.