Beyondtheir metallophore properties, lusichelins, particularlylusichelin B (2), exhibit promising anticancer potential.Lusichelin B (2) demonstrated potent cytotoxicity againstboth monolayer cultures and tumor spheroids of human colon carcinomaHCT 116 cells, and it effectively overcame cancer MDR by modulatingthe efflux activity of the ABCB1 transmembrane pump. Here, ABCB1 is linked to neoplasm.