Design and synthesis of pyrazole derivatives as potent and selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP)

…, S Narisawa, B Brown, JL Millan, E Sergienko…

文献索引：Sidique, Shyama; Ardecky, Robert; Su, Ying; Narisawa, Sonoko; Brown, Brock; Millan, Jose Luis; Sergienko, Eduard; Cosford, Nicholas D.P. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 1 p. 222 - 225

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被引用次数: 52

摘要

Tissue-nonspecific alkaline phosphatase (TNAP) plays a central role in regulating extracellular matrix calcification during bone formation and growth. High-throughput screening (HTS) for small molecule TNAP inhibitors led to the identification of hits in the sub- micromolar potency range. We report the design, synthesis and in vitro evaluation of a series of pyrazole derivatives of a screening hit which are potent TNAP inhibitors exhibiting IC50 ...