Synthesis and structure-activity relationship studies of CD4 down-modulating cyclotriazadisulfonamide (CADA) analogues

TW Bell, S Anugu, P Bailey, VJ Catalano…

文献索引：Bell, Thomas W.; Anugu, Sreenivasa; Bailey, Patrick; Catalano, Vincent J.; Dey, Kaka; Drew, Michael G. B.; Duffy, Noah H.; Jin, Qi; Samala, Meinrado F.; Sodoma, Andrej; Welch, William H.; Schols, Dominique; Vermeire, Kurt Journal of Medicinal Chemistry, 2006 , vol. 49, # 4 p. 1291 - 1312

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被引用次数: 27

摘要

HIV attachment via the CD4 receptor is an important target for developing novel approaches to HIV chemotherapy. Cyclotriazadisulfonamide (CADA) inhibits HIV at submicromolar levels by specifically down-modulating cell-surface and intracellular CD4. An effective five-step synthesis of CADA in 30% overall yield is reported. This synthesis has also been modified to produce more than 50 analogues. Many tail-group analogues have been made by ...