tetano
Editor, Senior Moderator
Chem Biodivers. 2015 Apr;12(4):685-96. doi: 10.1002/cbdv.201400337.
[h=1]Novel daidzein analogs and their in vitro anti-influenza activities.[/h] Chung ST[SUP]1[/SUP], Huang YT, Hsiung HY, Huang WH, Yao CW, Lee AR.
[h=3]Author information[/h]
[h=3]Abstract[/h] A series of novel isoflavonoids were synthesized based on structural modifications of daidzein, an active ingredient of traditional Chinese medicine (TCM) and evaluated for their anti-influenza activity, in vitro, against H1N1 Tamiflu-resistant (H1N1 TR) virus in the MDCK cell line. Among them, 4-oxo-4H-1-benzopyran-8-carbaldehydes 11a-11g were most promising, and they demonstrated better activities and selectivities comparable to those the reference ribarivin, a nucleoside antiviral agent. 3-(4-Bromophenyl)-7-hydroxy-4-oxo-4H-1-benzopyran-8-carboxaldehyde (11c) displayed the best inhibitory activity (EC50 , 29.0 μM) and selectivity index (SI>10.3). Analysis of the structureactivity relationships (SAR) indicated that both the non-naturally-occurring Br-substituted B-ring and appropriate CHO and OH groups on the A-ring might be critical for the activity and selectivity against H1N1 TR influenza viruses.
Copyright ? 2015 Verlag Helvetica Chimica Acta AG, Z?rich.
[h=4]KEYWORDS:[/h] Anti-influenza virus; Daidzein; H1N1 Tamiflu-resistant virus; Isoflavonoids
PMID: 25879510 [PubMed - in process]
[h=1]Novel daidzein analogs and their in vitro anti-influenza activities.[/h] Chung ST[SUP]1[/SUP], Huang YT, Hsiung HY, Huang WH, Yao CW, Lee AR.
[h=3]Author information[/h]
[h=3]Abstract[/h] A series of novel isoflavonoids were synthesized based on structural modifications of daidzein, an active ingredient of traditional Chinese medicine (TCM) and evaluated for their anti-influenza activity, in vitro, against H1N1 Tamiflu-resistant (H1N1 TR) virus in the MDCK cell line. Among them, 4-oxo-4H-1-benzopyran-8-carbaldehydes 11a-11g were most promising, and they demonstrated better activities and selectivities comparable to those the reference ribarivin, a nucleoside antiviral agent. 3-(4-Bromophenyl)-7-hydroxy-4-oxo-4H-1-benzopyran-8-carboxaldehyde (11c) displayed the best inhibitory activity (EC50 , 29.0 μM) and selectivity index (SI>10.3). Analysis of the structureactivity relationships (SAR) indicated that both the non-naturally-occurring Br-substituted B-ring and appropriate CHO and OH groups on the A-ring might be critical for the activity and selectivity against H1N1 TR influenza viruses.
Copyright ? 2015 Verlag Helvetica Chimica Acta AG, Z?rich.
[h=4]KEYWORDS:[/h] Anti-influenza virus; Daidzein; H1N1 Tamiflu-resistant virus; Isoflavonoids
PMID: 25879510 [PubMed - in process]