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The synthesis is described of 1-chloromethyl-5-hydroxy-1, 2-dihydro-3H-benz [e] indole (seco- CBI)- pyrrole polyamide conjugates (1-4) which were labeled with a fluorescent Fmoc moiety to evaluate their cellular uptake. Confocal laser scanning microscopy (CLSM) indicates that these DNA minor groove-binding agents localize in the cytoplasm and organelles.