Abstract: The discovery of antitumor activity of cisplatin has prompted the search for new metallic complexes as potential anticancer drugs. Among them, gold complexes have gained increasing attention as anticancer drugs. The obvious antiproliferative effect caused by alkynylphosphine gold(Ⅰ) complex stems from its novel mechanism of action. At the same time, alkynylphosphine gold(Ⅰ) complex has become one of the hot spots in the field of gold-based anticancer drugs for the future due to its unique chemical properties and related coordination modes. This review summarizes the research progress of antitumor activity of alkynylphosphine gold(Ⅰ) complexes in recent years, including the structural characteristics, optimal design, synergistic efficacy, diagnostic and therapeutic activity, in the hope of providing reference for related research and application.