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4-(acylaminomethyl)benzamides were prepared in two steps from 4-aminomethylbenzoic acid and assayed in the NCl's primary anti-cancer screen. Eight out of 34 compounds showed interesting antiproliferative activity. From these compounds, three were selected for further in vivo testing. In addition, all the compounds were tested against farnesyltransferase and the cell cycle regulating enzymes cdc2 kinase and cdc25 phosphatase. The compounds proved inactive in these assays, as were some selected compounds in an assay searching for possible interference with the ras/raf interaction in a yeast two-hybrid system.