Low-dimensional nanomaterials (LDNs) are receiving increasing attention in cancert herapy owing to their unique properties, especially the large surfacea rea-tovolume ratio. LDNs such as metallicn anoparticles (NPs), hydroxyapatite NPs, graphene derivatives, and black phosphorus (BP) nanosheets have been proposed for drug delivery, photothermal/photodynamic therapies, andm ultimodal theranostict reatments. The therapeutic effectiveness is mainly based on the physical characteristics of LDNs, but their inherent bioactivity has not been fully capitalized. In this Minireview,r ecent advances in the anti-cancer effects of varioust ypes of LDNs with inherentc hemotherapeutic bioactivity are described and the bioactivity mechanismsa re discussed on the cellular and molecular levels.B P, one of the newesta nd exciting members of the LDN family,i sh ighlighted owing to the excellent inherent bioactivity,s electivity,a nd biocompatibility in cancert herapy.L DNs and related derivatives possess inherentb ioactivity and selective chemotherapeutic effects suggesting large potentiala sn anostructured anti-cancer agentsinc ancer therapy.