Quinone‐based N‐sulfonyl‐1,2,3‐triazoles were synthesized by click chemistry and subsequently evaluated against eight types of cancer cell lines. Some of the compounds exhibited potent cytotoxicity with IC50 values < 1.0 μM. Also, the cytotoxic potential of the quinones was evaluated against peripheral blood mononuclear (PBMC) and V79 cells. Additionally, the chemical reactivity of Rh(II) aza‐vinyl carbenes generated in situ from these triazoles was studied. These compounds could provide promising new lead derivatives for more potent anticancer drug development.
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