A series of novel indazole derivatives of Sirt 1 activator as osteogenic regulators

[Display omitted] A series of indazole derivatives were identified as Sirt 1 activators though high-throughput screening. Optimization of each substituent on the indazole ring led to the identification of compound 13. Compound 13 appeared to give the best Sirt 1 activity of the compounds tested and...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2017-11, Vol.27 (21), p.4828-4831
Main Authors: Atobe, Masakazu, Yamakawa, Natsumi, Wada, Yasuhiro, Goto, Tokuhito, Kawanishi, Masashi, Ito, Takeshi, Saito, Makoto, Takeda, Masahiro, Tabata, Takanori, Arai, Hirokazu
Format: Article
Language:English
Subjects:
Acetylation - drug effects
Cell Differentiation - drug effects
Cell Line
HTS
Humans
Indazole
Indazoles - chemistry
Indazoles - metabolism
Indazoles - pharmacology
Osteogeneration
Osteogenesis - drug effects
Osteoporosis
Sirt 1
Sirtuin 1 - chemistry
Sirtuin 1 - metabolism
Structure-Activity Relationship
Tumor Suppressor Protein p53 - metabolism
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Summary:[Display omitted] A series of indazole derivatives were identified as Sirt 1 activators though high-throughput screening. Optimization of each substituent on the indazole ring led to the identification of compound 13. Compound 13 appeared to give the best Sirt 1 activity of the compounds tested and also showed osteogenesis activity in a cell assay. Sirt 1 activators are therefore potential candidates for the treatment of osteoporosis.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2017.09.049