In search of non-platinum based anticancer drugs, we have synthesized and characterized a new class of three gadoliniumand a carbon nanotube composite, 1@CNT 4. The three oligopeptides, L 1 -L 3 were prepared in a novel synthetic route using tetramethyl benzotriazolyl uronium hexaflurophosphate (HBTU) as a peptide coupling reagent. Confocal microscopic analysis of the gadolinium(III)-oligopeptides, 1, 2 and CNT composite, 1@CNT 4 indicate that they display white and green light emissions upon excitations at λ, 405 and 488 nm with characteristic patterns. The oligopeptides, L 1 & L 3 display in vitro anticancer activity on HeLa cells with IC 50 values in one mM concentration whereas the IC 50 of RGD-based oligopeptide was found to be 1 μM. The IC 50 of gadolinium(III)-oligopeptide, 1 and the CNT composite, 4 were found to be 1 μM and 10 nM. The transmission electron microscopic investigation of the HeLa cells treated with the composite 4 confirm the cellular uptake and indicate the presence of CNTs in the cytoplasm and that CNTs appear like bullets carrying the gadolinium(III)-triaspartate, 1.