Discovery and validation of a series of aryl sulfonamides as selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP)

…, A Mangravita-Novo, M Vicchiarelli…

文献索引：Dahl, Russell; Sergienko, Eduard A.; Su, Ying; Mostofi, Yalda S.; Yang, Li; Simao, Ana Maria; Narisawa, Sonoko; Brown, Brock; Mangravita-Novo, Arianna; Vicchiarelli, Michael; Smith, Layton H.; O'Neill, W. Charles; Millan, Jose Luis; Cosford, Nicholas D. P. Journal of Medicinal Chemistry, 2009 , vol. 52, # 21 p. 6919 - 6925

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被引用次数: 41

摘要

We report the characterization and optimization of drug-like small molecule inhibitors of tissue-nonspecific alkaline phosphatase (TNAP), an enzyme critical for the regulation of extracellular matrix calcification during bone formation and growth. High-throughput screening (HTS) of a small molecule library led to the identification of arylsulfonamides as potent and selective inhibitors of TNAP. Critical structural requirements for activity were ...