- 5-Carba-pterocarpens: A new scaffold with anti-HCV activity
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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 H
- Fernandes, Talita de A.,Costa, Paulo R. R.,Manvar, Dinesh,Basu, Amartya,Kaushik-Basu, Neerja,Domingos, Jorge L. O.,Nichols, Daniel Brian
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- Synthesis and biological evaluation of α-aryl-α-tetralone derivatives as hepatitis C virus inhibitors
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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).
- Manvar, Dinesh,Fernandes, Talita De A.,Domingos, Jorge L.O.,Baljinnyam, Erdenechimeg,Basu, Amartya,Junior, Eurides F.T.,Costa, Paulo R.R.,Kaushik-Basu, Neerja
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supporting information
p. 51 - 54
(2015/02/19)
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- Synthesis of 5-carbapterocarpens by α-arylation of tetralones followed by one-pot demethylation/cyclization with BBr3
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5-Carbapterocarpens, one of them displaying estrogenic activity, were prepared from α-aryltetralones in high yields through a one-pot, BBr 3-promoted O-demethylation and cyclization sequence. The key α-aryltetralone intermediates were obtained
- Fernandes, Talita De A.,Domingos, Jorge L. O.,Da Rocha, Luiza I. A.,De Medeiros, Sabrina,Najera, Carmen,Costa, Paulo R. R.
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p. 1314 - 1320
(2014/03/21)
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- Synthesis of 5-Carbapterocarpens by α-Arylation of Tetralones Followed by One-Pot Demethylation/Cyclization with BBr3
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5-Carbapterocarpens, one of them displaying estrogenic activity, were prepared from α-aryltetralones in high yields through a one-pot, BBr3-promoted O-demethylation and cyclization sequence. The key α-aryltetralone intermediates were obtained b
- Fernandes, Talita De A.,Domingos, Jorge L. O.,Da Rocha, Luiza I. A.,De Medeiros, Sabrina,Njera, Carmen,Costa, Paulo R. R.
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p. 1314 - 1320
(2015/10/05)
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- Tetracyclic compounds as estrogen ligands
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This invention provides estrogen receptor modulators having the structure: wherein R1, R2, R3, R4, Q, n, R8, R9, R10, and R11 have been defined in the specification; o
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Page/Page column 11; 16
(2010/02/15)
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