title: Discovery of indeno[1,2-c]quinoline derivatives as inhibitors of osteoclastogenesis induced by receptor activator of NF-κB ligand (RANKL).
abstract: Certain indeno[1,2-c]quinolines were synthesized and evaluated for antiosteoclastogenic activities. Among them, 6,9-dimethoxy-11H-indeno[1,2-c]quinolin-11-one (8a) and 9-methoxy-6-(methylthio)-11H-indeno[1,2-c]quinolin-11-one (16a) inhibited RANKL-induced osteoclast formation in Raw 264.7 cells with an IC(50) of 2.00 and 2.58 μM, respectively. Compound 8a was only weakly active in the inhibition of the RANKL-induced NFAT activation, while 16a was inactive. These results indicated that the antiosteoclastogenic effect of 8a is only partly related while 16a is not related to the suppression of NFAT.
authors: Department of Medicinal and Applied Chemistry, College of Life Science, Kaohsiung Medical University, Kaohsiung City, Taiwan. tzengch@kmu.edu.tw
authors: Chih-Hua
authors: CH
authors: Tseng
authors: Ru-Wei
authors: RW
authors: Lin
authors: Yeh-Long
authors: YL
authors: Chen
authors: Gwo-Jaw
authors: GJ
authors: Wang
authors: Mei-Ling
authors: ML
authors: Ho
authors: Cherng-Chyi
authors: CC
authors: Tzeng
mesh_terms: D055808:Drug Discovery; D006801:Humans; D007192:Indenes / Q000494:pharmacology*; D010010:Osteoclasts / Q000187:drug effects* / Q000378:metabolism; D011804:Quinolines / Q000494:pharmacology*; D053245:RANK Ligand / Q000502:physiology*
chemical_list: D007192:Indenes; D011804:Quinolines; D053245:RANK Ligand; C505688:TNFSF11 protein, human