Robustaflavone, a naturally occurring biflavanoid, is a potent non-nucleoside inhibitor of hepatitis B virus replication in vitro

A Comparative Study of Bacteriostatic Activity of Synthetic Hydroxylated Flavonoids

“…Thus, research and use of these compounds as antioxidants (2,10,16), antimutagenic (6,7) and antibacterial (1,17), as well as their vasodilator effects (9), antiallergic activity (3), antidiabetic effect (15) and antiviral action (8) are very important.…”

Structure-Activity Relationship Study of Biflavonoids on the Dengue Virus Polymerase DENV-NS5 RdRp

“…Among the tested biflavonoids, six were isolated from D. araucarioides (Podocarpaceae), another endemic gymnosperm from New Caledonia (5)(6)(7)(8)(9)(10), one was obtained by hemisynthesis (11), and one was commercially purchased (12). Apigenin (13) and ten related flavonoid monomers (14-23) were also tested on the DENV-NS5 RdRp.…”

“…We previously demonstrated that biflavonoids from Dacrydium balansae, an endemic gymnosperm from New Caledonia, are potent inhibitors of the Dengue virus NS5 RNA-dependent RNA polymerase. Herein we describe the structure-activity relationship study of 23 compounds: biflavonoids from D. balansae (1-4) and from D. araucarioides (5-10), hexamethyl-amentoflavone (11), cupressuflavone (12), and apigenin derivatives (13)(14)(15)(16)(17)(18)(19)(20)(21)(22)(23). We conclude that 1) over the four different biflavonoid skeletons tested, amentoflavone (1) and robustaflavone (5) are the most promising ones for antidengue drug development, 2) the number and position of methyl groups on the biflavonoid moiety modulate their inhibition of Dengue virus NS5 RNA-dependent RNA polymerase, and 3) the degree of oxygena-tion of flavonoid monomers influences their antidengue potential.…”

Synthesis and biological assay of 4-aryl-6-chloro-quinoline derivatives as novel non-nucleoside anti-HBV agents

“…Most compounds exhibited moderate inhibitory activity against the secretion of HBsAg and HBeAg. Nine compounds (3,5,6,7,10,14,17,20,24) showed significant inhibition against HBV DNA replication with IC 50 values in the range of 4.4-9.8 lM, which were comparative to that of positive control tenofovir. Of them, compounds 10, 17, and 20 had low cytotoxicities, resulting in high SI values, >551.2, >143.7, and >284.5, respectively.…”

“…6,7 So far, non-nucleosides have also been reported to inhibit HBV infection. [7][8][9][10][11][12][13][14][15][16][17][18] Nevertheless, the search for compounds with novel anti-HBV target and mechanism is still a fascinating topic.…”