title: Synthesis and evaluation of 1-(benzo[b]thiophen-2-yl)ethanone analogues as novel anti-osteoporosis agents acting on BMP-2 promotor.
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).
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, People's Republic of China.
authors.forename: Zong-ying
authors.initials: ZY
authors.lastname: Liu
authors.forename: Xiao-bo
authors.initials: XB
authors.lastname: He
authors.forename: Zhao-yong
authors.initials: ZY
authors.lastname: Yang
authors.forename: Hua-yi
authors.initials: HY
authors.lastname: Shao
authors.forename: Xue
authors.initials: X
authors.lastname: Li
authors.forename: Hui-fang
authors.initials: HF
authors.lastname: Guo
authors.forename: Yue-qin
authors.initials: YQ
authors.lastname: Zhang
authors.forename: Shu-yi
authors.initials: SY
authors.lastname: Si
authors.forename: Zhuo-rong
authors.initials: ZR
authors.lastname: Li
mesh_terms: D000818:Animals; D055396:Bone Morphogenetic Protein 2 / Q000378:metabolism*; D001842:Bone and Bones / Q000473:pathology; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D005260:Female; D005786:Gene Expression Regulation; D006801:Humans; D051379:Mice; D008956:Models, Chemical; D010024:Osteoporosis / Q000188:drug therapy*; D010052:Ovariectomy; D011401:Promoter Regions, Genetic; D051381:Rats; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D055396:Bone Morphogenetic Protein 2; D013876:Thiophenes