Search Results - "Rault, S"

Target fishing reveals PfPYK-1 and PfRab6 as potential targets of an antiplasmodial 4-anilino-2-trichloromethylquinazoline hit compound by Kieffer, C., Primas, N., Hutter, S., Merckx, A., Reininger, L., Bach, S., Ruchaud, S., Gaillard, F., Laget, M., Amrane, D., Hervé, L., Castera-Ducros, C., Renault, J., Dumètre, A., Rault, S., Doerig, C., Rathelot, P., Vanelle, P., Azas, N., Verhaeghe, P.

“…[Display omitted] We present investigations about the mechanism of action of a previously reported 4-anilino-2-trichloromethylquinazoline antiplasmodial…”
Get full text

Targeting the BH3 domain of Bcl-2 family proteins. A brief history from natural products to foldamers as promising cancer therapeutic avenues by De Giorgi, M, Voisin-Chiret, A S, Rault, S

“…For many years the spotlight in drug discovery has been on a relatively small number of validated therapeutic target classes, such as G-protein coupled…”
Get more information

Synthesis and biological evaluation of novel pyrrolopyrrolizinones as anticancer agents by Rochais, C., Lisowski, V., Dallemagne, P., Rault, S.

“…We herein describe the synthesis of novel 3-(het)aryl-pyrrolo[2,3- b]pyrrolizin-8(1 H)-ones starting from commercial (het)aryl-acetonitriles. A more convergent…”
Get full text

Rapid and soft formulation of folate-functionalized nanoparticles for the targeted delivery of tripentone in ovarian carcinoma by Tomasina, J., Poulain, L., Abeilard, E., Giffard, F., Brotin, E., Carduner, L., Carreiras, F., Gauduchon, P., Rault, S., Malzert-Fréon, A.

“…We report the development of folate-functionalized nanoparticles able to target folate receptors, and to deliver a poorly water soluble cytotoxic agent, a…”
Get full text

New Risk Assessment Approach for Systemic Insecticides:  The Case of Honey Bees and Imidacloprid (Gaucho) by Halm, Marie-Pierre, Rortais, A, Arnold, G, Taséi, J. N, Rault, S

“…The procedure to assess the risk posed by systemic insecticides to honey bees follows the European Directives and depends on the determination of the Hazard…”
Get full text

Partial least squares analysis and mixture design for the study of the influence of composition variables on lipidic nanoparticle characteristics by Malzert-Fréon, A, Hennequin, D, Rault, S

“…Lipidic nanoparticles (NP), formulated from a phase inversion temperature process, have been studied with chemometric techniques to emphasize the influence of…”
Get more information

Molecular basis of agonist docking in a human GPR103 homology model by site‐directed mutagenesis and structure–activity relationship studies by Neveu, C, Dulin, F, Lefranc, B, Galas, L, Calbrix, C, Bureau, R, Rault, S, Chuquet, J, Boutin, J A, Guilhaudis, L, Ségalas‐Milazzo, I, Vaudry, D, Vaudry, H, Santos, J Sopkova‐de Oliveira, Leprince, J

“…Background and Purpose The neuropeptide 26RFa and its cognate receptor GPR103 are involved in the control of food intake and bone mineralization. Here, we have…”
Get full text

Influence of the introduction of a solubility enhancer on the formulation of lipidic nanoparticles with improved drug loading rates by Malzert-Fréon, A., Saint-Lorant, G., Hennequin, D., Gauduchon, P., Poulain, L., Rault, S.

“…The objective of the present paper is to develop lipidic nanoparticles (NP) able to encapsulate drugs presenting limited solubility in both water and lipids,…”
Get full text

Formulation of sustained release nanoparticles loaded with a tripentone, a new anticancer agent by Malzert-Fréon, A., Vrignaud, S., Saulnier, P., Lisowski, V., Benoît, J.P., Rault, S.

“…The purpose of the present work is to develop nanoparticles of a new antitubulin agent of the family of tripentones by means of a phase inversion process…”
Get full text

Reactivity of 3-Iodoimidazo[1,2-a]pyridines Using a Suzuki-Type Cross-Coupling Reaction by Enguehard, Cécile, Renou, Jean-Louis, Collot, Valérie, Hervet, Maud, Rault, Sylvain, Gueiffier, Alain

“…The influence of base and solvent in Suzuki cross-coupling reaction on various 2-substituted-3-iodoimidazo[1,2-a]pyridines was reported. The reactivity was…”
Get full text

Efficient Synthesis of Novel 3-(Het)arylanthranilic Acids via a Suzuki Cross-Coupling Reaction of 7-Iodoisatin with (Het)arylboronic Acids in Water by Lisowski, Vincent, Robba, Max, Rault, Sylvain

Get full text

Prediction of the fish acute toxicity from heterogeneous data coming from notification files by Faucon, J.C., Bureau, R., Faisant, J., Briens, F., Rault, S.

“…Four descriptors (Molecular weight, log(Pow), hardness and free energy of solvation) were selected to predict, on a training set of heterogeneous chemical…”
Get full text

New aromatase inhibitors. Synthesis and biological activity of aryl-substituted pyrrolizine and indolizine derivatives by SONNET, P, DALLEMAGNE, P, SOURDAINE, P, SERALINI, G.-E, GUILLON, J, ENGUEHARD, C, STIEBING, S, TANGUY, A. J, BUREAU, A. R, RAULT, A. S, AUVRAY, A. P, MOSLEMI, S

“…We report herein the design and the synthesis of some aryl-substituted pyrrolizine and indolizine derivatives, on the basis of a hypothetical pharmacophore…”
Get full text

Synthesis of New 2-(Aminomethyl)-4-phenylpyrrolo[1,2-a]-quinoxalines and their Preliminary In-vivo Central Dopamine Antagonist Activity Evaluation in Mice by GUILLON, J., BOULOUARD, M., LISOWSKI, V., STIEBING, S., LELONG, V., DALLEMAGNE, P., RAULT, S.

“…In the search for antipsychotic agents that are not associated with extrapyramidal side effects, efforts have been focused on finding selective D4‐receptor…”
Get full text

Applicability of CATALYST in Ecotoxicology, a New Promising Tool for 3D-QSAR: Study of Chlorophenols by Briens, F., Bureau, R., Rault, S.

“…With the aim of applying recent quantitative structure–activity relationship (QSAR) descriptors coming from the pharmaceutical sciences to the modelization of…”
Get full text

Synthesis of novel pyrazolopyrrolopyrazines, potential analogs of sildenafil by Kopp, Marina, Lancelot, Jean-Charles, Dallemagne, Patrick, Rault, Sylvain

“…Synthesis of novel pyrazolopyrrolopyrazines is herein described with the aim to reach new specific PDE‐5 inhibitors of potential clinical interest in male…”
Get full text

Prediction of the Daphnia acute toxicity from heterogeneous data by Faucon, J.C., Bureau, R., Faisant, J., Briens, F., Rault, S.

“…Two descriptors (log( P ow), ‘hardness’) were selected to predict the Daphnia acute toxicity of a training set of heterogeneous chemical compounds. The data…”
Get full text

Synthesis and preliminary behavioural evaluation in mice of new 3-aryl-3-pyrrol-1-ylpropanamides, analogues of FGIN-1-27 and FGIN-1-43 by Guillon, J., Boulouard, M., Lelong, V., Dallemagne, P., Rault, S., Jarry, C.

“…The 2‐aryl‐3‐indoleacetamides FGIN‐1–27 and FGIN‐1–43 have already been characterized in‐vitro as potent and specific ligands for the mitochondrial DBI…”
Get full text

Design and synthesis of a new type of non steroidal human aromatase inhibitors by Sonnet, P., Guillon, J., Enguehard, C., Dallemagne, P., Bureau, R., Rault, S., Auvray, P., Moslemi, S., Sourdaine, P., Galopin, S., Séralini, G.-E.

“…The structure-activity relationship study of one of recently described aromatase inhibitors, compound 1 (MR20814), allowed us to design some related…”
Get full text

Medicinal chemistry within the Atlantic Arc and collaboration within Franco-Belges pharmacochemistry by Rault, Sylvain, Blagbrough, Ian S

Get full text