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  • Discovery of indeno[1,2-c]quinoline derivatives as inhibitors of osteoclastogenesis induced by receptor activator of NF-κB ligand (RANKL).

Discovery of indeno[1,2-c]quinoline derivatives as inhibitors of osteoclastogenesis induced by receptor activator of NF-κB ligand (RANKL).

Journal of medicinal chemistry (2011-04-05)
Chih-Hua Tseng, Ru-Wei Lin, Yeh-Long Chen, Gwo-Jaw Wang, Mei-Ling Ho, Cherng-Chyi Tzeng
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
(−)-Epigallocatechin gallate, ≥95%
Sigma-Aldrich
(−)-Epigallocatechin gallate, ≥80% (HPLC), from green tea