| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1395401 | European Journal of Medicinal Chemistry | 2015 | 4 Pages |
•α-Aryl-α-tetralones are prepared through direct palladium catalyzed α-arylation.•The anti-HCV activity of α-aryl-α-tetralones (1-carba-isoflavanones) is reported.•LQB314 is the most potent and selective against HCV genotype 1b (IC50 1.8 μM, SI > 111).•LQB307 is the most potent and selective against HCV genotype 2a (IC50 1.5 μM, SI > 101).
The synthesis of a novel series of 1-carba-isoflavanones through the α-arylation of α-tetralones is described. Several of these compounds demonstrated potent activity and selectivity in-vitro against HCV replicon reporter cells. Compound 10 (LQB-314) exhibited the best profile being active and selective in both replicon reporter cells (IC50 1.8 μM, SI > 111 and IC50 4.3 μM, SI > 46 in Huh7/Rep-Feo1b and Huh7.5-FGR-JC1-Rluc2A, respectively). Compound 3 (LQB-307) was the more potent and selective for Huh7.5-FGR-JC1-Rluc2A replicon reporter cells (IC50 1.5 μM, SI > 101.4).
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