Discovery of quercetin derivatives as metal ions chelators with potent anti-HCV activities

ZHONG Dongwei; LIU Mingming; CAO Yang; ZHOU Lu; YE Deyong

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Discovery of quercetin derivatives as metal ions chelators with potent anti-HCV activities

ZHONG Dongwei,LIU Mingming,CAO Yang,ZHOU Lu,YE Deyong * #

School of Pharmacy, Fudan University, Shanghai 201203

*Correspondence author

#Submitted by

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Funding: Chinese National Natural Science Foundation （No.Grants No. 81373330）, National Drug Innovative Program （No.No. 2009ZX09301- 011）, Chinese Ministry of Education （No.No. 20130071110068）

Opened online:16 May 2017

Accepted by: none

Citation: ZHONG Dongwei,LIU Mingming,CAO Yang.Discovery of quercetin derivatives as metal ions chelators with potent anti-HCV activities[OL]. [16 May 2017] http://en.paper.edu.cn/en_releasepaper/content/4730625

The α,γ-diketoacid (DKA) analogues or isosteres show potent inhibition of hepatitis C virus (HCV) NS5B polymerase through chelation of the two magnesium ions at the active site. The anti-HCV activity of flavonoid quercetin (2) could partly be attributed to its structural mimic of DKAs. In order to delineate the structural features required for the inhibitory effect and improve the anti-HCV potency, two novel quercetin analogues, 7-O-arylmethyl quercetin and quercetin-3-O-benzoic acid-ester, were designed, synthesized and evaluated for their anti-HCV properties in cell-based assays. Among the 38 newly synthesized compounds, 7-O-substituted derivative 3i and 3-O-substituted derivative 4f were found to be the most active in corresponding series (EC50 = 3.8 μM and 9.0 μΜ, respectively). Docking studies suggested that the quercetin analogues are capable of establishing key coordination with the two magnesium ions as well as interactions with residues at the active site of HCV NS5B.

Keywords:anti-HCV activities; diketoacids mimic; quercetin derivatives; synthesis; docking

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