103438-85-3Relevant articles and documents
Benzylideneacetone Derivatives Inhibit Osteoclastogenesis and Activate Osteoblastogenesis Independently Based on Specific Structure-Activity Relationship
Pativada, Triveni,Kim, Myung Hwan,Lee, Jung-Hun,Hong, Seong Su,Choi, Chun Whan,Choi, Yun-Hyeok,Kim, Woo Jung,Song, Da-Woon,Park, Serk In,Lee, Eun Jung,Seo, Bo-Yeon,Kim, Hankyeom,Kim, Hong Kyu,Lee, Kee Ho,Ahn, Sung K.,Ku, Jin-Mo,Park, Gil Hong
, p. 6063 - 6082 (2019)
(E)-3,4-Dihydroxybenzylideneacetone (compound 1) inhibited receptor activator of NF-κB ligand-induced osteoclastogenesis of C57BL/6 bone marrow monocyte/macrophages with IC50 of 7.8 μM (IC50 of alendronate, 3.7 μM) while stimulating the differentiation of MC3T3-E1 osteoblastic cells, accompanied by the induction of Runt-related transcription factor 2, alkaline phosphatase, and osteocalcin. (E)-4-(3-Hydroxy-4-methoxyphenyl)-3-buten-2-one (compound 2c) showed a dramatically increased osteoclast-inhibitory potency with IC50 of 0.11 μM while sustaining osteoblast-stimulatory activity. (E)-4-(4-Hydroxy-3-methoxyphenyl)-3-buten-2-one (compound 2g) stimulated alkaline phosphatase production 2-fold at 50 μM without changing osteoclast-inhibitory activity, compared with compound 1. Oral administration of compounds 1, 2c, and 2g prevented ovariectomy-induced osteoporosis in ddY mice to a degree proportional to their osteoclastogenesis-inhibitory potencies. The administration of 1 (mg/kg)/d compound 2c ameliorated histomorphometry of osteoporotic bone to a degree comparable with 10 (mg/kg)/d alendronate. Conclusively, the in vitro capacity of a few benzylideneacetone derivatives to inhibit osteoclastogenesis supported by independent osteoblastogenesis activation was convincingly reflected in in vivo management of osteoporosis, suggesting a potential novel therapeutics for osteopenic diseases.
NOVEL COMPOUNDS, USES AND METHODS FOR THEIR PREPARATION
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Paragraph 00341, (2018/03/06)
The present disclosure relates to novel compounds HIF-2α inhibitors and pharmaceutical compositions thereof which may be useful in the treatment and/or prevention of various conditions. The present disclosure also provides methods of preparing such HIF-2α inhibitors and compositions, and methods of using the same.
Sanglifehrin Derivatives and Methods for Their Production
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Paragraph 0150; 0151, (2014/04/03)
There are provided inter alia compounds of formula (I) and (II) and their use in therapy, particularly for the treatment of viral infection.