Wyniki wyszukiwania dla: Jean-Pierre Hénichart

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Eaton’s Reagent‐Mediated Domino π‐Cationic Arylations of Aromatic Carboxylic Acids to Iasi‐Red Polymethoxylated Polycyclic Aromatic Hydrocarbons: Products with Unprecedented Biological Activities as Tubulin Polymerization Inhibitors

Alina Ghinet, Philippe Gautret, Nathalie Van Hijfte, Bertrand Ledé, więcej

Chemistry – A European Journal > 20 > 32 > 10117 - 10130

A rapid domino π‐cationic arylation of aromatic carboxylic acids, mediated by Eaton’s reagent, has been developed for the synthesis of Iasi‐red polymethoxylated polycyclic aromatic hydrocarbons (PAHs). This route is currently the easiest method to obtain such popular PAH compounds, which bear in addition numerous methoxy groups. The domino process was generalized, the structure of the obtained red...

artykuł

Studies on pyrrolidinones. synthesis of fused 1,5-naphthyridines

Rufine Akué-Gédu, Daniel Couturier, Jean-Pierre Hénichart, Benoît Rigo, więcej

Tetrahedron > 2012 > 68 > 27-28 > 5644-5654

The synthesis of new condensed indolizinediones derived from pyroglutamic acid is described. The Semmler–Wolff transposition of the oxime of these ketones leads to fused dihydro-1,5-naphthyridinones. Easy introduction of side amino chains indicates that potential DNA-intercalating heterocyclic systems fused on 1,5-naphthyridine nucleus could be obtained in these series.

artykuł

Studies on pyrrolidinones. Synthesis of 4,5-fused-3-hydroxypyridinyl-2-propionic acid derivatives

Rufine Akué-Gédu, Daniel Couturier, Jean-Pierre Hénichart, Benoit Rigo, więcej

Tetrahedron > 2012 > 68 > 4 > 1117-1127

The synthesis of some condensed indolizinediones derived from pyroglutamic acid is described. Treatment of these ketones in HCl, HBr or MeONa/MeOH furnished aryl propionic acid derivatives. During the ketone transformations, two sequential processes could take place in competitive manner to provide heterocyclic systems bearing carboxylic acid or hydroxycarboxylic acid function. Easy synthesis of amides...

artykuł

Synthesis and biological evaluation of phenstatin metabolites

Alina Ghinet, Benoît Rigo, Jean-Pierre Hénichart, Delphine Le Broc-Ryckewaert, więcej

Bioorganic & Medicinal Chemistry > 2011 > 19 > 20 > 6042-6054

Previous investigations on the incubation of phenstatin with rat and human microsomal fractions revealed the formation of nine main metabolites. The structures of eight of these metabolites have been now confirmed by synthesis and their biological properties have been reported. Eaton’s reagent was utilized as a convenient condensing agent, allowing, among others, a simple multigram scale preparation...

artykuł

Toward new camptothecins. Part 7: Synthesis of thioluotonin and its 5-methoxycarbonyl derivative

Thomas Boisse, Laurent Gavara, Philippe Gautret, Brigitte Baldeyrou, więcej

Tetrahedron Letters > 2011 > 52 > 14 > 1592-1596

The synthesis of thiodeoxyvasicinone and thioluotonin derivatives is described. The results obtained indicate that in these series, oxygen to sulfur replacement leads to absence of strong interaction with topoisomerase I-DNA.

artykuł

Toward new camptothecins. Part 6: Synthesis of crucial ketones and their use in Friedländer reaction

Laurent Gavara, Thomas Boisse, Jean-Pierre Hénichart, Adam Daïch, więcej

Tetrahedron > 2010 > 66 > 38 > 7544-7561

In the context of the preparation of camptothecin and luotonin A analogs, the synthesis of some key keto-precursors and their use in Friedländer condensation are described. This paper also focuses on the stability of these keto intermediates and emphasizes the major differences between indolizinones and pyrroloquinazolinones series. Noteworthy is also the report of some original structures isolated...

artykuł

Synthesis and biological activity of N-aroyl-tetrahydro-γ-carbolines

Alexandre Bridoux, Régis Millet, Jean Pommery, Nicole Pommery, więcej

Bioorganic & Medicinal Chemistry > 2010 > 18 > 11 > 3910-3924

Research on dual inhibitors of both 5-LOX and COXs gained interest due to the overexpressions of these enzymes during the malignant state of the evolution of prostate cancer. In order to take part in this research, new N-aroyl-tetrahydro-γ-carbolines issued from the modification of Indomethacin have been synthesised. As for the NSAIDs, the compounds have been tested for their activity against COX...

artykuł

Studies on pyrrolidinones. On the application of copper-catalyzed arylation of methyl pyroglutamate to obtain a new benzo[de]quinoline scaffold

Alina Ghinet, Souhila Oudir, Jean-Pierre Hénichart, Benoît Rigo, więcej

Tetrahedron > 2010 > 66 > 1 > 215-221

Optimized conditions for copper-catalyzed N-arylation of methyl pyroglutamate are described. These studies permitted the synthesis of methyl N-naphthylpyroglutamate, which was then cyclized to a ketone. The known dehydration of amidoketones by PPA was extended to this new scaffold to lead to a novel condensed benzo[de]quinoline with potential antioxidative activity.

artykuł

2,6-Diphenylthiazolo[3,2-b][1,2,4]triazoles as telomeric G-quadruplex stabilizers

Jamal El Bakali, Frédérique Klupsch, Aurore Guédin, Bertrand Brassart, więcej

Bioorganic & Medicinal Chemistry Letters > 2009 > 19 > 13 > 3434-3438

The design and synthesis of 2,6-diphenylthiazolo[3,2-b][1,2,4]triazoles characterized by a large aromatic building block bearing cationic side chains are reported. These molecules are evaluated as telomeric G-quadruplex stabilizers and for their selectivity towards duplex DNA by competition experiments. Two compounds (14a, 19) were found active with high selectivity for telomeric G-quadruplex over...

artykuł

Toward new camptothecins. Part 5: On the synthesis of precursors for the crucial Friedländer reaction

Thomas Boisse, Laurent Gavara, Jean-Pierre Hénichart, Benoît Rigo, więcej

Tetrahedron > 2009 > 65 > 12 > 2455-2466

The synthesis of potential precursors of ketones, which could be used to obtain camptothecin analogs, is described. Noteworthy is the difference of reactivity between indolizinone and pyrrolidinoquinazolinone heterocycle.

artykuł

Synthesis and biological evaluation of a new family of anti-benzylanilinosulfonamides as CA IX inhibitors

Anne Thiry, Aurélie Delayen, Laurence Goossens, Raymond Houssin, więcej

European Journal of Medicinal Chemistry > 2009 > 44 > 2 > 511-518

We report the synthesis and the pharmacological evaluation of a new class of human carbonic anhydrase (hCA) inhibitors prepared regio- and stereoselectively by reacting sulfanilamide with ethyl trans-phenylglycidate in the presence of cobalt(II) chloride. Various derivatizations of the ester moiety in the parent compound led to a small library of derivatives (2R,3R and 2S,3S) which displayed interesting...

artykuł

New NSAIDs-NO hybrid molecules with antiproliferative properties on human prostatic cancer cell lines

Nicolas Bézière, Laurence Goossens, Jean Pommery, Hervé Vezin, więcej

Bioorganic & Medicinal Chemistry Letters > 2008 > 18 > 16 > 4655-4657

The design of profen hybrids containing a NO donor moiety connected to an aliphatic spacer led to compounds with a similar cyclooxygenase inhibition compared to their parent profen and with significant antiproliferative activities on PC3 cells. However, inhibition of COX-2 pathway alone did not seem sufficient to inhibit cancer cell proliferation, and NO-release in a time-dependent manner strongly...

artykuł

A new synthesis of pyrrolo[3,2-b]quinolines by a tandem electrocyclization–oxidation process

Thomas Boisse, Philippe Gautret, Benoît Rigo, Laurence Goossens, więcej

Tetrahedron > 2008 > 64 > 30-31 > 7266-7272

A new synthesis of pyrrolo[3,2-b]quinolines is described. Condensation of anilines with dimethyl 4-oxopyrrolidine-1,3-dicarboxylate yields enaminoesters, which upon reaction with Bredereck's reagent produce the title compounds. A possible reaction mechanism is briefly discussed.

artykuł

Synthesis, Cytotoxicity, DNA Interaction, and Topoisomerase II Inhibition Properties of Novel Indeno[2,1- c ]quinolin-7-one and Indeno[1,2- c ]isoquinolin-5,11-dione Derivatives

Adina Ryckebusch, Deborah Garcin, Amélie Lansiaux, Jean-François Goossens, więcej

Journal of Medicinal Chemistry > 2008 > 51 > 12 > 3617 - 3629

artykuł

Synthesis and biological activities of a series of 4,5-diaryl-3-hydroxy-2(5H)-furanones

Fabrice Bailly, Clémence Queffélec, Gladys Mbemba, Jean-François Mouscadet, więcej

European Journal of Medicinal Chemistry > 2008 > 43 > 6 > 1222-1229

A series of thirteen 4,5-diaryl-3-hydroxy-2(5H)-furanones were synthesized. They were evaluated for their antioxidant potencies and inhibitory properties of 5-lipoxygenase, cyclooxygenases, HIV-1 integrase and PC3 cell proliferation. New hits were discovered either in the antiproliferation test or in the HIV anti-integrase test.

artykuł

A new method of bromination of aromatic rings by an iso-amyl nitrite/HBr system

Laurent Gavara, Thomas Boisse, Benoît Rigo, Jean-Pierre Hénichart

Tetrahedron > 2008 > 64 > 22 > 4999-5004

A mixture of iso-amyl nitrite/HBr is shown to be a mild and efficient reagent for electrophilic aromatic bromination. The reaction succeeds with slightly activated arenes and heterocyclic compounds. By using HCl instead of HBr, chlorination can also be performed in few cases. The i-amONO ₂ /HBr mixture can also be utilized for bromination in the α-position of electron withdrawing groups. A...

artykuł

Pharmacomodulations around the 4-Oxo-1,4-dihydroquinoline-3-carboxamides, a Class of Potent CB ₂ -Selective Cannabinoid Receptor Ligands: Consequences in Receptor Affinity and Functionality

Eric Stern, Giulio G. Muccioli, Barbara Bosier, Laurie Hamtiaux, więcej

Journal of Medicinal Chemistry > 2007 > 50 > 22 > 5471 - 5484

artykuł

From dicarbonylallene to 1-aryl-3,6-dimethyl-4-aminoaryl-2-pyridones: a one-pot versatile and uncatalyzed synthesis

Thomas Boisse, Benoît Rigo, Régis Millet, Jean-Pierre Hénichart

Tetrahedron > 2007 > 63 > 42 > 10511- 10520

Reaction of amines with an allenic precursor leads to new 1-aryl-3,6-dimethyl-4-aminoaryl-2-pyridones in good yields. These syntheses can be performed in two distinct steps, allowing the possibility to introduce different substituents in the positions 1 and 4. By using o-aminopyridine, a new pyridopyrimidone is easily obtained.

artykuł

Design, synthesis and biological evaluation of substituted dioxodibenzothiazepines and dibenzocycloheptanes as farnesyltransferase inhibitors

Pauline Gilleron, Nicolas Wlodarczyk, Raymond Houssin, Amaury Farce, więcej

Bioorganic & Medicinal Chemistry Letters > 2007 > 17 > 19 > 5465-5471

A new series of FTase inhibitors containing a tricyclic moiety—dioxodibenzothiazepine or dibenzocycloheptane—has been designed and synthesized. Among them, dioxodibenzothiazepine 18d displayed significant inhibitory FTase activity (IC ₅₀ =17.3nM) and antiproliferative properties.

artykuł

Toward new camptothecins. Part 4: On the reactivity of nitro and amino precursors of aza analogs of 5-methoxycarbonyl camptothecin

Laurent Gavara, Benoît Rigo, Daniel Couturier, Laurence Goossens, więcej

Tetrahedron > 2007 > 63 > 38 > 9456-9464

In the context of formation of new aza analogs of camptothecin, nitration then reduction of condensed pyridones was realized, leading to new derivatives of pyrrolo-aza-indoles. Treatment of these compounds with hydrobromic acid led to new structure rearrangements while oxidation of the α-position was unsuccessful. Mechanisms of formation of the new products are discussed.

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