About @rtMolecule
Founded at Poitiers (France) in 2003, @rtMolecule is a private incorporated company, specialized in custom chemical synthesis of compounds that are not commercially available. Our expertise includes Stable isotopes, Metabolites, Impurities, APIs and key intermediates, micropollutants or emerging pollutants for use as analytical standards in bioanalytical assay (pharmaceutical and environmental context). In addition to custom synthesis @rtMolecule is also engaged in pharmacomodulation of active compounds, in production of screening compounds and building blocks.
Publications
- Superacid‐Mediated Late‐Stage Aromatic Polydeuteration of Pharmaceuticals
E Appert, A Martin‐Mingot, O Karam… - … A European Journal, 2022 - Wiley Online Library
The field of medicinal chemistry is currently witnessing a deuterium rush owing to the
remarkable properties of this element as bioisoster of hydrogen atom. Aromatic hydrogen … - Complementary Site-Selective Sulfonylation of Aromatic Amines by Superacid Activation
P Bourbon, E Appert, A Martin-Mingot, B Michelet… - Organic …, 2021 - ACS Publications
Under superacidic conditions, aniline and indole derivatives are sulfonylated at low
temperature with easy-to-access arenesulfonic acids or arenesulfonyl hydrazides. By … - Complementary Site‐Selective Halogenation of Nitrogen‐Containing (Hetero) Aromatics with Superacids
A Mamontov, A Martin‐Mingot… - … A European Journal, 2020 - Wiley Online Library
Site‐selective functionalization of arenes that is complementary to classical aromatic
substitution reactions remains a long‐standing quest in organic synthesis. Exploiting the … - Superacid‐Catalyzed Trifluoromethylthiolation of Aromatic Amines
LJC Bonazaba Milandou, H Carreyre… - Angewandte Chemie …, 2017 - Wiley Online Library
Upon activation under superacid conditions, functionalized tailor‐made N‐SCF3
sulfenamides served as reagents for the trifluoromethylthiolation of aromatic amines. This - Inside Back Cover: Superacid-Catalyzed Trifluoromethylthiolation of Aromatic Amines (Angew. Chem. Int. Ed. 1/2017).
LJC Bonazaba Milandou, H Carreyre… - Angewandte …, 2017 - search.ebscohost.com
Superacid activation of N‐SCF3 sulfenamide reagents generates diprotonated
superelectrophilic species for the trifluoromethylthiolation of aromatic amines, as shown by … - Tandem superelectrophilic activation for the regioselective chlorofluorination of recalcitrant allylic amines
A Le Darz, U Castelli, N Mokhtari, A Martin-Mingot… - Tetrahedron, 2016 - Elsevier
An efficient and straightforward regio-controlled route to β-fluoro-γ-chlorinated amines was
developed via an ammonium–chloronium superelectrophilic activation in superacid HF/SbF … - Fluorinated pyrrolidines and piperidines incorporating tertiary benzenesulfonamide moieties are selective carbonic anhydrase II inhibitors
Le Darz, A Mingot, F Bouazza, U Castelli… Journal of Enzyme …, 2015 - Taylor & Francis
A series of substituted pyrrolidines and piperidines were synthesized using superacid HF/SbF5 chemistry. Investigated as inhibitors of several human carbonic anhydrase (hCA, EC 4.2.… - 42nd congress of the “Groupe Français des Pesticides”(French Group of Pesticide research-GFP 2012)
JF Cholleta, M Couderchetb, JL Bonnemainc - researchgate.net
The 42nd congress of the" Groupe Français des Pesticides"(French Group of Pesticide
research-GFP 2012) took place May 30-June 1 at the" École Nationale Supérieure … - Superelectrophilic activation in superacid HF/SbF5 and synthesis of benzofused sultams
F Liu, A Martin-Mingot, MP Jouannetaud… - Organic …, 2010 - ACS Publications
The synthesis of benzofused sultams and/or fluorinated sulfonamides, starting from N-allylic
sulfonamides, was performed in superacid HF/SbF5, through superelectrophilic activation. A … - 42nd Congress of the “Groupe Français des Pesticides”(French Group of Pesticide research–GFP 2012) ENSIP, Poitiers, France, 30 May–1 June 2012
JF Chollet, M Couderchet, JL Bonnemain - Environmental Science and …, 2014 - Springer
The 42nd congress of the “Groupe Français des Pesticides”(French Group of Pesticide
research–GFP 2012) took place 30 May–1 June at the “École Nationale Supérieure … - Synthesis of fluorinated nitrogen-containing compounds in superacid HF/SbF5
S Thibaudeau, G Compain, F Liu, A Martin-Mingot, M Jouannetaud, ...
11th International Biorelated Polymer Symposium/243rd National Spring … - Substitution effect on the hydrofluorination reaction of unsaturated amines in superacid HF/SbF 5
F Liu, A Martin-Mingot, MP Jouannetaud… - Organic & …, 2009 - pubs.rsc.org
This paper describes the scope and limitations of the hydrofluorination reaction in superacid
HF/SbF5. On the basis of experimental studies of polyfunctional substrates' behaviour, the … - Fluorinated pyrrolidines and piperidines incorporating tertiary benzenesulfonamide moieties are selective carbonic anhydrase II inhibitors
A Le Darz, A Mingot, F Bouazza, U Castelli… - Journal of Enzyme …, 2015 - Taylor & Francis
A series of substituted pyrrolidines and piperidines were synthesized using superacid
HF/SbF5 chemistry. Investigated as inhibitors of several human carbonic anhydrase (hCA … - Selective synthesis of gem-chlorofluorinated nitrogen-containing derivatives after superelectrophilic activation in superacid HF/SbF5
F Liu, A Martin-Mingot, MP Jouannetaud… - The Journal of …, 2011 - ACS Publications
The first direct selective synthesis of novel gem-chlorofluorinated nitrogen-containing
building blocks in superacid is reported. The dramatic role of the chlorine atom on the … - A novel, facile route to β-fluoroamines by hydrofluorination using superacid HF–SbF5
S Thibaudeau, A Martin-Mingot… - Chemical …, 2007 - pubs.rsc.org
A novel, facile route to β-fluoroamines by hydrofluorination using superacid HF – SbF5 -
Chemical Communications (RSC Publishing) DOI:10.1039/B703629A Royal Society of … - Efficient oxidative ipso-fluorination of para-substituted phenols using pyridinium polyhydrogen fluoride in combination with hypervalent iodine (III) reagents
O Karam, A Martin-Mingot, MP Jouannetaud, JC Jacquesy, A Cousson
Tetrahedron 60 (31), 6629-6638 - An efficient synthesis of 6-hydroxymelatonin, a human metabolite of melatonin
O Karam, F Zunino, V Chagnaut, MP Jouannetaud, JC Jacquesy
Tetrahedron letters 44 (7), 1511-1513
Product Citations
- An easily expandable multi-drug LC-MS assay for the simultaneous quantification of 57 oral antitumor drugs in human plasma
N Kehl, K Schlichtig, P Dürr, L Bellut, F Dörje, R Fietkau… - Cancers, 2021 - mdpi.com
… Next, [ 2 H 4 ]-olaparib was purchased from Biomol (Hamburg, Germany), and [ 2 H 3 ]-clopidogrel
was bought from @rt molecule (Poitiers, France). Dimethyl sulfoxide (DMSO), water, … - ALK-transformed mature T lymphocytes restore early thymus progenitor features
A Congras, C Hoareau-Aveilla, N Caillet… - The Journal of …, 2020 - Am Soc Clin Investig
Anaplastic large cell lymphoma (ALCL) is a mature T cell neoplasm that often expresses the
CD4+ T cell surface marker. It usually harbors the t (2; 5)(p23; q35) translocation, leading to … - Contrôle de l'expression de Bcl-2 dans les lymphomes anaplasiques à grandes cellules par la protéine HuR en réponse au crizotinib: impact sur l'apoptose …
A Torossian - 2017 - theses.hal.science
Les lymphomes anaplasiques à grandes cellules (LAGC) sont des lymphomes non-
hodgkiniens dits de type T ou nul, représentant la majorité des lymphomes T pédiatriques … - High levels of mir-7-5p potentiate crizotinib-induced cytokilling and autophagic flux by targeting raf1 in npm-alk positive lymphoma cells
D Sorrentino, J Frentzel, G Mitou, RB Blasco… - Cancers, 2020 - mdpi.com
Simple Summary Anaplastic lymphoma kinase positive anaplastic large cell lymphomas are
a pediatric disease, which still needs treatment improvement. Crizotinib was the first ALK … - Targeting autophagy enhances the anti-tumoral action of crizotinib in ALK-positive anaplastic large cell lymphoma
G Mitou, J Frentzel, A Desquesnes, S Le Gonidec… - Oncotarget, 2015 - ncbi.nlm.nih.gov
Abstract Anaplastic Lymphoma Kinase-positive Anaplastic Large Cell Lymphomas (ALK+
ALCL) occur predominantly in children and young adults. Their treatment, based on … - Analyse de traces de micropolluants dans l'eau et le lait maternel en vue d'évaluer leur impact sur la santé
PS RABOUAN - core.ac.uk
Je tiens à remercier Madame Nathalie KARPEL VEL LEITNER, directeur de recherche au
CNRS de m'avoir accueillie dans l'équipe Eaux, Sols, Santé, Environnement. Ces travaux … - Increased oral bioavailability of resveratrol by its encapsulation in casein nanoparticles
R Peñalva, J Morales, CJ González-Navarro… - International journal of …, 2018 - mdpi.com
Resveratrol is a naturally occurring polyphenol that provides several health benefits
including cardioprotection and cancer prevention. However, its biological activity is limited … - Overexposure to bisphenol A and its chlorinated derivatives of patients with end-stage renal disease during online hemodiafiltration
A Bacle, A Dupuis, M Belmouaz, M Bauwens… - Biomolecules, 2019 - mdpi.com
The health safety conditions governing the practice of online hemodiafiltration (OL-HDF) do
not yet incorporate the risks related to the presence of endocrine disruptors such as … - Adaptive phenotype of microglial cells during the normal postnatal development of the somatosensory “Barrel” cortex
I Arnoux, M Hoshiko, L Mandavy, E Avignone… - Glia, 2013 - Wiley Online Library
Accumulative evidence indicates that microglial cells influence the normal development of
central nervous system (CNS) synapses. Yet, the functional properties of microglia in … - The effect of route of administration on the enantioselective pharmacokinetics of ketamine and norketamine in rats
M Le Nedelec, P Glue, H Winter… - Journal of …, 2018 - journals.sagepub.com
Background: Ketamine has been shown to produce a rapid and potent antidepressant
response in patients with treatment-resistant depression. Currently ketamine is most … - In vitro primary human and animal cell-based blood− brain barrier models as a screening tool in drug discovery
O Lacombe, O Videau, D Chevillon… - Molecular …, 2011 - ACS Publications
Brain penetration is characterized by its extent and rate and is influenced by drug
physicochemical properties, plasma exposure, plasma and brain protein binding and BBB … - Evaluation of seven drug metabolisms and clearances by cryopreserved human primary hepatocytes cultivated in microfluidic biochips
R Baudoin, JM Prot, G Nicolas, J Brocheton… - Xenobiotica, 2013 - Taylor & Francis
We present characterization of the metabolic performance of human cryopreserved
hepatocytes cultivated in a platform of parallelized microfluidic biochips. The RTqPCR … - Mild Regioselective Halogenation of Anilines, Anilides, and Indoles
V Snieckus, CE Brown, MA Reed - Synfacts, 2020 - thieme-connect.com
Significance: The prevalence of halogenated arenes in pharmaceuticals and agrochemicals
necessitates mild procedures for late-stage functionalization of N-heterocycles. Here, a site … - Online monitoring of hepatic rat metabolism by coupling a liver biochip and a mass spectrometer
F Merlier, R Jellali, E Leclerc - Analyst, 2017 - pubs.rsc.org
A microfluidic liver biochip was coupled with a mass spectrometer to detect in real time the
drug metabolism of hepatocytes. The hepatocytes were cultivated in the biochip for 35 h … - Blockade of crizotinib-induced BCL2 elevation in ALK-positive anaplastic large cell lymphoma triggers autophagy associated with cell death
A Torossian, N Broin, J Frentzel, C Daugrois… - …, 2019 - ncbi.nlm.nih.gov
Anaplastic lymphoma kinase (ALK)-positive anaplastic large cell lymphomas are tumors that
carry translocations involving the ALK gene at the 2p23 locus, leading to the expression of … - Biological monitoring of human exposure to neonicotinoids using urine samples, and neonicotinoid excretion kinetics
KH Harada, K Tanaka, H Sakamoto, M Imanaka… - PloS one, 2016 - journals.plos.org
Background Neonicotinoids, which are novel pesticides, have entered into usage around
the world because they are selectively toxic to arthropods and relatively non-toxic to … - Neonicotinoid concentrations in urine from chronic kidney disease patients in the North Central Region of Sri Lanka
R Kabata, S Nanayakkara… - journal of …, 2016 - Wiley Online Library
Neonicotinoid concentrations in urine from chronic kidney disease patients in the North
Central Region of Sri Lanka: Risako Kabata, et al. Department of Health and Environmental … - Simultaneous quantification of trans-resveratrol and its sulfate and glucuronide metabolites in rat tissues by stable isotope-dilution UPLC–MS/MS analysis
BS Lou, PS Wu, CW Hou, F Cheng, JK Chen - Journal of Pharmaceutical …, 2014 - Elsevier
A rapid, sensitive, and selective ultra performance liquid chromatography–tandem mass
spectrometry (UPLC–MS/MS) in the multiple reaction monitoring (MRM) mode has been … - A cocktail of metabolic probes demonstrates the relevance of primary human hepatocyte cultures in a microfluidic biochip for pharmaceutical drug screening
JM Prot, O Videau, C Brochot, C Legallais… - International journal of …, 2011 - Elsevier
In this paper, we compare the biotransformation capacities of cryopreserved primary human
hepatocytes cultivated in a liver microfluidic biochip and in plates. The hepatocytes were … - Reliable quantification of bisphenol A and its chlorinated derivatives in human urine using UPLC–MS/MS method
N Venisse, C Grignon, B Brunet, S Thévenot, A Bacle… - Talanta, 2014 - Elsevier
Bisphenol A (BPA), a widespread man-made chemical classified as an endocrine disruptor,
is increasingly considered as a major cause of concern for human health. Chlorine present … - Ubiquitous occurrence of chlorinated byproducts of bisphenol A and nonylphenol in bleached food contacting papers and their implications for human exposure
Y Zhou, M Chen, F Zhao, D Mu… - … Science & Technology, 2015 - ACS Publications
The occurrence of bisphenol A (BPA), nonylphenol (NP), and their six chlorinated
byproducts were investigated in 74 food contacting papers (FCPs) from China, the USA … - Development and validation of a liquid-chromatography high-resolution tandem mass spectrometry approach for quantification of nine cytochrome P450 (CYP) model …
J Dinger, MR Meyer, HH Maurer - Analytical and bioanalytical chemistry, 2014 - Springer
Abstract Knowledge about the cytochrome P450 (CYP) inhibition potential of new drug
candidates is important for drug development because of its risk of interactions. For novel … - In vitro cytochrome P450 inhibition potential of methylenedioxy-derived designer drugs studied with a two-cocktail approach
J Dinger, MR Meyer, HH Maurer - Archives of toxicology, 2016 - Springer
In vitro cytochrome P450 (CYP) inhibition assays are common approaches for testing the
inhibition potential of drugs for predicting potential interactions. In contrast to marketed … - Ultrasensitive determination of bisphenol A and its chlorinated derivatives in urine using a high-throughput UPLC-MS/MS method
C Grignon, N Venisse, S Rouillon, B Brunet… - Analytical and …, 2016 - Springer
Bisphenol A (BPA) is a well-known endocrine disruptor. Chlorinated derivatives of BPA
(ClxBPA) may be formed by reaction of chlorine with BPA present in drinking water. ClxBPA … - Cytochrome P450 inhibition potential of new psychoactive substances of the tryptamine class
J Dinger, C Woods, SD Brandt, MR Meyer, HH Maurer - Toxicology letters, 2016 - Elsevier
New psychoactive substances (NPS) are not tested for their cytochrome P450 (CYP)
inhibition potential before consumption. Therefore, this potential was explored for tryptamine … - Development of an in vitro cytochrome P450 cocktail inhibition assay for assessing the inhibition risk of drugs of abuse
J Dinger, MR Meyer, HH Maurer - Toxicology letters, 2014 - Elsevier
Drugs of abuse are not tested for cytochrome P450 (CYP) inhibition potential before
distribution. Therefore, a cocktail assay should be developed for testing the inhibition … - Zein-based nanoparticles improve the oral bioavailability of resveratrol and its anti-inflammatory effects in a mouse model of endotoxic shock
R Penalva, I Esparza, E Larraneta… - Journal of agricultural …, 2015 - ACS Publications
Resveratrol offers pleiotropic health benefits including a reported ability to inhibit
lipopolysaccharide (LPS)-induced cytokine production. The aim of this work was to prepare … - Metrology in Environment and Biology: The case of Nonylphenols in Environmental Health
S Rabouan, A Dupuis, A Cariot, M Albouy-Llaty… - 2012 - hal.science
Over recent decades, the development of environmental risks along with their repercussions
on health has led to the appearance of a scientific research field of environmental health in … - Analytical chemistry and metrological issues related to nonylphenols in environmental health
S Rabouan, A Dupuis, A Cariot, M Albouy-Llaty… - TrAC Trends in …, 2012 - Elsevier
In recent decades, the development of environmental risks and their repercussions on
health has led to environmental health being a field of scientific research in which … - Doxorubicin-induced loss of DNA topoisomerase II and DNMT1-dependent suppression of MiR-125b induces chemoresistance in ALK-positive cells
A Congras, N Caillet, N Torossian, C Quelen… - Oncotarget, 2018 - ncbi.nlm.nih.gov
Systemic anaplastic large-cell lymphoma (ALCL) is a childhood T cell neoplasm defined by
the presence or absence of translocations that lead to the ectopic expression of anaplastic … - Biochemical and analytical development of the CIME cocktail for drug fate assessment in humans
O Videau, M Delaforge, M Levi… - Rapid …, 2010 - Wiley Online Library
Phenotyping based on drug metabolism activity appears to be informative regarding