Synthesis, biological evaluation and 3D-QSAR studies of 3-keto salicylic acid chalcones and related amides as novel HIV-1 integrase inhibitors

…, S Patil, TW Sanchez, N Neamati, RF Schinazi…

文献索引：Sharma, Horrick; Patil, Shivaputra; Sanchez, Tino W.; Neamati, Nouri; Schinazi, Raymond F.; Buolamwini, John K. Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 6 p. 2030 - 2045

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被引用次数: 52

摘要

HIV-1 integrase is one of the three most important enzymes required for viral replication and is therefore an attractive target for anti retroviral therapy. We herein report the design and synthesis of 3-keto salicylic acid chalcone derivatives as novel HIV-1 integrase inhibitors. The most active compound, 5-bromo-2-hydroxy-3-[3-(2, 3, 6-trichlorophenyl) acryloyl] benzoic acid (25) was selectively active against integrase strand transfer, with an IC50 of ...