- Synthesis of new α-Aryl-α-tetralones and α-Fluoro-α-aryl-α-tetralones, preliminary antiproliferative evaluation on drug resistant cell lines and in silico prediction of ADMETox properties
-
α-aryl-α-tetralones and α-fluoro-α-aryl-α-tetralones derivatives were synthesized by palladium catalyzed α-arylation reaction of α-tetralones and α-fluoro-α-tetralones, with bromoarenes in moderate to good yields. These compounds were evaluated for their
- de Souza, Luana G.,Salustiano, Eduardo J.,da Costa, Kelli M.,Costa, Angela T.,Rumjanek, Vivian M.,Domingos, Jorge L.O.,Rennó, Magdalena N.,Costa, Paulo R.R.
-
-
- Palladate Precatalysts for the Formation of C-N and C-C Bonds
-
A series of imidazolium-based palladate precatalysts has been synthesized and the catalytic activity of these air- and moisture-stable complexes evaluated as a function of the nature of the imidazolium counterion. These precatalysts can be converted under
- Zinser, Caroline M.,Warren, Katie G.,Nahra, Fady,Al-Majid, Abdullah,Barakat, Assem,Islam, Mohammad Shahidul,Nolan, Steven P.,Cazin, Catherine S. J.
-
p. 2812 - 2817
(2019/08/12)
-
- Enantioselective electrophilic fluorination of α-aryl-tetralones using a preparation of N-fluoroammonium salts of cinchonine
-
The enantioselective electrophilic fluorination of α-aryl-tetralones is promoted by cinchonine/selectfluor combinations. This strategy allows a facile synthesis of the corresponding 2-fluoro-2-aryl-1-tetralones with excellent yields (up to >98%) and moder
- Souza, Luana G.,de O. Domingos, Jorge L.,de A. Fernandes, Talita,Renno, Magdalena N.,Sansano, Jose M.,Najera, Carmen,Costa, Paulo R.R.
-
-
- 5-Carba-pterocarpens: A new scaffold with anti-HCV activity
-
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
-
-
- Synthesis and biological evaluation of α-aryl-α-tetralone derivatives as hepatitis C virus inhibitors
-
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
-
supporting information
p. 51 - 54
(2015/02/19)
-
- Synthesis of 5-carbapterocarpens by α-arylation of tetralones followed by one-pot demethylation/cyclization with BBr3
-
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.
-
p. 1314 - 1320
(2014/03/21)
-
- Synthesis of 5-Carbapterocarpens by α-Arylation of Tetralones Followed by One-Pot Demethylation/Cyclization with BBr3
-
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.
-
p. 1314 - 1320
(2015/10/05)
-
- Suzuki-Miyaura, α-ketone arylation and dehalogenation reactions catalyzed by a versatile N-heterocyclic carbene-palladacycle complex
-
The activity of the complex (IPr)PdCl(η2-N,C-C 12H7NMe2), 1 [IPr = (N,N′-bis(2,6- diisopropylphenyl)-imidazol)-2-ylidene], in the Suzuki-Miyaura cross-coupling reaction involving unactivated aryl chlorides and triflates with arylboronic acids at room temperature in technical grade 2-propanol is described. These conditions allow for the synthesis of di- and tri-ortho-substituted biaryls in very short reaction times. This complex also displays very high activity for α-ketone arylation and dehalogenation reactions of activated and unactivated aryl chlorides.
- Navarro, Oscar,Marion, Nicolas,Oonishi, Yoshihiro,Kelly III, Roy A.,Nolan, Steven P.
-
p. 685 - 692
(2007/10/03)
-
- Inhibitors of acyl CoA:cholesterol acyltransferase
-
Conformational restriction of previously disclosed acyclic diphenylethyl)diphenylacetamides led to the discovery of several potent inhibitors of acyl CoA:cholesterol acyltransferase (ACAT). cis-[2-(4- Hydroxyphenyl)-1-indanyl]diphenylacetamide (4a) was the most potent ACAT inhibitor identified (IC50 = 0.04 μM in an in vitro rat hepatic microsomal ACAT assay, ED50 = 0.72 mg/kg/day in cholesterol-fed hamsters).
- Vaccaro, Wayne,Amore, Cindy,Berger, Joel,Burrier, Robert,Clader, John,Davis, Harry,Domalski, Martin,Fevig, Tom,Salisbury, Brian,Sher, Rosy
-
p. 1704 - 1719
(2007/10/03)
-