The present communication reveals out the interfacial antitumor mechanism of novel peptide anchored metal nanoparticles synthesized via phase-transfer route. The in vitro antitumor studies make obvious that the functionalized nanoparticles are good antitumorals. Further to confirm the antitumor mechanism, the authors put forth a DNA interrupting study of their functionalized nanoparticles with radical scavengers such as mannitol, DMSO, ethanol, methanol, and tert-butyl alcohol in the presence of glutathione reductase enzymatic system. This electrophoretic mobility shift assay results highly ensure the participation of hydroxyl anion and hydroxyl radical in the antitumoral action of the synthesized compounds.Supplemental materials are available for this article. Go to the publisher's online edition of Synthesis and Reactivity in Inorganic, Metal-Organic, and Nano-Metal Chemistry to view the supplemental file.