Synthesis and evaluation of Hsp90 inhibitors that contain the 1, 4-naphthoquinone scaffold

MK Hadden, SA Hill, J Davenport, RL Matts…

文献索引：Kyle Hadden; Hill, Stephanie A.; Davenport, Jason; Matts, Robert L.; Blagg, Brian S.J. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 2 p. 634 - 640

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被引用次数: 39

摘要

High-throughput screening of a library of diverse molecules has identified the 1, 4- naphthoquinone scaffold as a new class of Hsp90 inhibitors. The synthesis and evaluation of a rationally-designed series of analogues containing the naphthoquinone core scaffold has provided key structure–activity relationships for these compounds. The most active inhibitors exhibited potent in vitro activity with low micromolar IC50 values in anti- ...