Caldorazole () was isolated from the marine cyanobacterium sp. collected on Ishigaki Island, Okinawa, Japan. Its structure was determined to be a new polyketide that contained two thiazole rings and an -methylenolpyruvamide moiety. Caldorazole () showed strong cytotoxicity toward tumor cells that had been seeded at a high density. Cell death induced by in HeLa and A431 cells was also observed only in the presence of the glycolysis blocker 2-deoxy-d-glucose (2DG). Co-treatment with and 2DG remarkably decreased ATP levels in these cells. Furthermore, selectively inhibited complex I in the mitochondrial respiratory chain. Thus, was demonstrated to exert cytotoxicity toward human tumor cells by blocking mitochondrial respiration.
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