Pincer complexes featuring tunable tridentate ligand frameworks are one of the most actively studied classes of metal-based complexes. Currently, growing attention is devoted to the cytotoxicity of pincer and related metal complexes. The antiproliferative activity of numerous pincer complexes has been reported. Pincer tridentate ligand scaffolds show different coordination modes and offer multiple options for directed structural modifications. This review summarizes the significant progress in the research studies of the antitumor activity of pincer and related platinum(ii), gold(iii), palladium(ii), copper(ii), iron(iii), ruthenium(ii), nickel(ii) and some other metal complexes, in order to provide a reference for designing novel metal coordination drug candidates with promising antitumor activity.