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The Versatile Nature of the 6-Aminoquinolone Scaffold : Identification of Submicromolar Hepatitis C Virus NS5B Inhibitors
- Manfroni, Giuseppe (author)
- Cannalire, Rolando (author)
- Barreca, Maria Letizia (author)
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- Kaushik-Basu, Neerja (author)
- Leyssen, Pieter (author)
- Iraci, Nunzio (author)
- Manvar, Dinesh (author)
- Paeshuyse, Jan (author)
- Guhamazumder, Rupa (author)
- Basu, Amartya (author)
- Sabatini, Stefano (author)
- Tabarrini, Oriana (author)
- Neyts, Johan (author)
- Cecchetti, Violetta (author)
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- (creator_code:org_t)
- 2013-11-06
- 2014
- English.
- In: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 57:5, s. 1952-1963
- Journal article (peer-reviewed)
Abstract
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- We have previously reported that the 6-aminoquinolone chemotype is a privileged scaffold to obtain antibacterial and antiviral agents. Herein we describe the design, synthesis, and enzymatic and cellular characterization of new 6-aminoquinolone derivatives as potent inhibitors of NS5B polymerase, an attractive and viable therapeutic target to develop safe anti-HCV agents. The 6-amino-7-[4-(2-pyridinyl)-1-piperazinyl]quinolone derivative 8 proved to be the best compound of this series, exhibiting an IC50 value of 0.069 mu M against NS5B polymerase and selective antiviral effect (EC50 = 3.03 mu M) coupled with the absence of any cytostatic effect (CC50 > 163 mu M; SI > 54) in Huh 9-13 cells carrying a HCV genotype 1b, as measured by MTS assay. These results indicate that the 6-aminoquinolone scaffold is worthy of further investigation in the context of NS5B-targeted HCV drug discovery programs.
Subject headings
- NATURVETENSKAP -- Kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences (hsv//eng)
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- ref (subject category)
- art (subject category)
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