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The aim of this study was to employ the pharmacophore hybrid strategy to merge GA with various dithiocarbamates and obtain novel compounds with better antitumor activities. We present a two\u2010step synthetic protocol wherein the GA derivative underwent reaction with carbon disulfide and various secondary amines in a one\u2010pot manner under mild conditions, facilitating the preparation of a series of structurally novel GA\u2010dithiocarbamate derivatives. Bioassay screening revealed that the representative compound <jats:bold>3c<\/jats:bold> demonstrated the capacity to reduce the mitochondrial membrane potential in Hep3B and Huh\u20107 cells, induce nuclear apoptosis, inhibit invasion and migration, and prompt both early and late apoptosis. Furthermore, our research findings indicated that this apoptotic phenomenon may be associated with the expression of Bcl\u20102, Bax, Bak, PARP, and cleaved\u2010PARP proteins. 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