Abstract: In order to develop the HIV integrase inhibitors with high bioactivity、low toxicity and favorable bioavailability, several key DKAs (Diketo acids) integrase inhibitors are introduced to provide academic basis for searching effective anti-HIV medicine according to those medicines widely used in market. Many aspects are analyzed, such as the data of biological activites, pharmacophore, target design and clinic research. Further R&D direction is discussed, which can be references for developing Diketo acids inhibitors of HIV integrase.