5-Carba-pterocarpens: A new scaffold with anti-HCV activity
| Autor: | Paulo R. R. Costa, Talita de A. Fernandes, Dinesh Manvar, Amartya Basu, Jorge L.O. Domingos, Daniel Brian Nichols, Neerja Kaushik-Basu |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Scaffold Stereochemistry viruses Hepacivirus Anisoles Antiviral Agents Guanidines Catalysis Cell Line 03 medical and health sciences 0302 clinical medicine Drug Discovery Humans 030212 general & internal medicine Replicon Tetralones EC50 Pharmacology biology Anti hiv Chemistry Organic Chemistry General Medicine biochemical phenomena metabolism and nutrition biology.organism_classification Hepatitis C In vitro 030104 developmental biology Cell culture Selectivity Palladium |
| Zdroj: | European Journal of Medicinal Chemistry. 112:33-38 |
| ISSN: | 0223-5234 |
| Popis: | The synthesis of a series of 5-carba-pterocarpens derivatives involving the cyclization of α-aryl-α-tetralones is described. Several compounds demonstrated potent activity and selectivity in vitro against HCV replicon reporter cells. The best profile in Huh7/Rep-Feo1b replicon reporter cells was observed with 2h (EC50 = 5.5 μM/SI = 20), while 2e was the most active in Huh7.5-FGR-JC1-Rluc2A replicon reporter cells (EC50 = 1.5 μM/SI = 70). Hydroxy groups at A- and D-rings are essential for anti-HCV activity, and substitutions in the A-ring at positions 3 and 4 resulted in enhanced activity of the compounds. |
| Databáze: | OpenAIRE |
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