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HIV/AIDS pandemics is a serious threat to health and development of mankind, and searching for effective anti‐HIV agents remains actual. Considerable progress has been made in recent years in the field of drug development against HIV. A lot of structurally different coumarins were found to display potent anti‐HIV activity. The current review demonstrates the variety of synthetic coumarins having unique mechanism of action referring to the different stages of HIV replication. Recent studies based on the account of various synthetic coumarins seem to indicate that some of them serve as potent non‐nucleoside RT‐inhibitors, another as inhibitors of HIV‐integrase or HIV‐protease. The merits of selecting potential anti‐HIV agents to be used in rational combination drugs design and structure‐activity relationships are discussed.The scientific community is looking actively for new drugs and combinations for treatment of …