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Mono-, di- and polynuclear metal alkynyl or σ-acetylide complexes have attracted a great deal of interest due to their multi-dimensional applications. In the past few decades, several small to medium sized neutral and charged metal acetylides have been synthesized and assessed for various biomedical applications. This review explores the progress made in the design and development of rigid-rod type η¹-σ-alkynyl complexes for therapeutic (viz. anticancer, antibacterial) and diagnostic (viz. enzymes or proteins imaging) purposes. The features that make metal acetylides unique for bio-applications, their diversity as biomaterials, and future potential for clinical usage have been reviewed. Although few challenges exist with this class of materials (which we have identified and discussed in the review), metal acetylides have a bright future in different branches of medical science and hold promise as next generation …