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Ajoene is a natural allylsulfur compound found in crushed garlic that arrests growth and induces apoptosis in cancer cells. To gain mechanistic insights into the cytotoxicity of ajoene in cancer cells, two fluorescently labelled ajoene analogs with dansyl‐ (DP) and fluorescein‐ (FOX) tags were synthesized. The tagged ajoenes were found to retain their activity at inhibiting proliferation and inducing apoptosis in MDA‐MB‐231 human breast‐cancer and WHCO1 human esophageal‐cancer cells. Both tagged ajoenes localized to the endoplasmic reticulum (ER) in MDA‐MB‐231 cells as observed by live cell confocal laser scanning microscopy (CLSM) and confirmed by generating an MDA‐MB‐231 cell line expressing yellow fluorescent protein (YFP) in the ER. DP appears to S‐thiolate multiple protein targets in MDA‐MB‐231 cells as observed by immunoblotting under non‐reducing conditions only; and a competition …