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Benzoflavone activators of the cystic fibrosis transmembrane conductance regulator: towards a pharmacophore model for the nucleotide-binding domain

…, GO Berger, H Yang, CW Dicus, W Choung…

文献索引:Springsteel, Mark F.; Galietta, Luis J. V.; Ma, Tonghui; By, Kolbot; Berger, Gideon O.; Yang, Hong; Dicus, Christopher W.; Choung, Wonken; Quan, Chao; Shelat, Anang A.; Guy, R. Kiplin; Verkman; Kurth, Mark J.; Nantz, Michael H. Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 18 p. 4113 - 4120

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被引用次数: 51

摘要

Our previous screen of flavones and related heterocycles for the ability to activate the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel indicated that UCCF-029, a 7, 8-benzoflavone, was a potent activator. In the present study, we describe the synthesis and evaluation, using cell-based assays, of a series of benzoflavone analogues to examine structure–activity relationships and to identify compounds having ...

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