Discovery and structure–activity relationship of thienopyridine derivatives as bone anabolic agents

…, A Nakao, T Shinozuka, K Shimada, S Matsui…

文献索引：Saito, Keiji; Nakao, Akira; Shinozuka, Tsuyoshi; Shimada, Kousei; Matsui, Satoshi; Oizumi, Kiyoshi; Yano, Kazuki; Ohata, Keiko; Nakai, Daisuke; Nagai, Yoko; Naito, Satoru Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 7 p. 1628 - 1642

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被引用次数: 8

摘要

A cell-based assay was performed for the discovery of novel bone anabolic agents. Alkaline phosphatase (ALPase) activity of ST2 cells was utilized as an indicator of osteoblastic differentiation, and thienopyridine derivative 1 was identified as a hit compound. 3- Aminothieno [2, 3-b] pyridine-2-carboxamide was confirmed to be a necessary core structure for the enhancement of ALPase activity, and then optimization of the C4-substituent on the ...