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A series of novel <i>N</i>²-acryloylhydrazides <b>1a–m</b> and a related series of compounds <b>6a–c</b> were prepared as potential chemostimulants. In general, these compounds are cytotoxic to human HCT 116 colon cancer cells, as well as human MCF-7 and MDA-MB-231 breast cancer cell lines. A representative compound <i>N</i>¹-(3,4-dimethoxyphenylcarbonyl)-<i>N</i>²-acryloylhydrazine <b>1m</b> sensitized HCT 116 cells to the potent antineoplastic agent 3,5-bis(benzylidene)-4-piperidone <b>2a</b>, and also to 5-fluorouracil. A series of compounds was prepared that incorporated some of the molecular features of <b>2a</b> and related compounds with various <i>N</i>²-acryloylhydrazides in series 1. These compounds are potent cytotoxins. Two modes of action of representative compounds are the lowering of mitochondrial membrane potential and increasing the concentration of reactive oxygen species.