Bioorganic & Medicinal Chemistry Letters 2009-08-01

Synthesis and evaluation of 1-(benzo[b]thiophen-2-yl)ethanone analogues as novel anti-osteoporosis agents acting on BMP-2 promotor.

Zong-ying Liu, Xiao-bo He, Zhao-yong Yang, Hua-yi Shao, Xue Li, Hui-fang Guo, Yue-qin Zhang, Shu-yi Si, Zhuo-rong Li

Index: Bioorg. Med. Chem. Lett. 19 , 4167-70, (2009)

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Abstract

A novel series of 1-(benzo[b]thiophen-2-yl)ethanone analogues were prepared and evaluated for enhancing BMP-2 expression. Compounds 1-5, 7, 8, 12, 13 and 16, with upregulation rate values of 35.6%, 27.9%, 39.8%, 32.0%, 37.1%, 30.2%, 28.0%, 33.5%, 22.8% and 27.3% in vitro, respectively, at a concentration of 4muM, exhibited potent effect for enhancing BMP-2 expression. We also found that compounds 1 and 12 produced a dose-dependent increase on bone histology and histomorphometry, and effectively reduced bone defects induced by ovariectomy in an ovariectomized rat model (OVX).