Monodisperse Fe(3)O(4) nanoparticles (NPs) originally synthesized with a hydrophobic oleylamine capping ligand were made water soluble and conjugated to the anticancer drug Methotrexate (MTX) using a new chemistry based on the readily available linker trichloro-s-triazine (TsT). This new linker is much more versatile than those that currently exist for attaching biomolecules to magnetic NPs. The MTX-conjugated NPs were found to be stable under physiological conditions for over 72 hours and MTX was shown to maintain its anticancer activity after conjugation to the NP surface. Through cell viability studies and intracellular uptake studies, MTX-conjugated NPs were shown to have targeting specificity for a tumor cell line (9L rat glioma) over a healthy cell line (Cultured Pulmonary Artery Endothelial). Additionally the MTX-conjugated NPs were visualized inside 9L cells using fluorescence microscopy to help elucidate their path within a cell after internalization.