Christophe Rochais

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Documents

Publications

Publications

Shaping Future Medicinal Chemists: Perspectives from European Schools of Pharmacy within the GP 2 A Network

Gülşah Bayraktar , Laura Carro , Michael Decker , Francesca Giuntini , Jean-Jacques Helesbeux et al.
Journal of Medicinal Chemistry, 2025, 68 (3), pp.2045-2047. ⟨10.1021/acs.jmedchem.4c03103⟩
Article dans une revue hal-04950824 v1
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Evidence from a mouse model supports repurposing an anti-asthmatic drug, bambuterol, against Alzheimer’s disease by administration through an intranasal route

Anne-Claire Groo , Thomas Curel , Aurélie Malzert-Fréon , Line Séguy , Ophélie Bento et al.
Communications Biology, 2025, 8 (1), pp.155. ⟨10.1038/s42003-025-07599-7⟩
Article dans une revue hal-04927352 v1

Indirect influence on the BDNF/TrkB receptor signaling pathway via GPCRs, an emerging strategy in the treatment of neurodegenerative disorders

Mirjana Antonijevic , Patrick Dallemagne , Christophe Rochais
Medicinal Research Reviews, 2025, 45 (1), pp.274-310. ⟨10.1002/med.22075⟩
Article dans une revue hal-04893240 v1

Implication of Central β 2 Adrenergic Receptor for the Development of Novel Drugs Against Alzheimer's Disease

Alice Wang , Marc Since , Patrick Dallemagne , Christophe Rochais
Archiv der Pharmazie / Chemistry in Life Sciences, 2025, 358 (4), ⟨10.1002/ardp.202400750⟩
Article dans une revue hal-05020271 v1

Anti-Breast Cancer Properties and In Vivo Safety Profile of a Bis-Carbazole Derivative

Jessica Ceramella , Camillo Rosano , Domenico Iacopetta , Iméne Ben Toumia , Leila Chekir-Ghedira et al.
Pharmaceutics, 2025, 17 (4), pp.415. ⟨10.3390/pharmaceutics17040415⟩
Article dans une revue hal-05014835 v1

Analysis of skeletal diversity of multi-target directed ligands (MTDLs) targeting Alzheimer's disease

Uzma Azam , Muhammad Moazzam Naseer , Christophe Rochais
European Journal of Medicinal Chemistry, 2025, 286, pp.117277. ⟨10.1016/j.ejmech.2025.117277⟩
Article dans une revue hal-04912969 v1
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Inducing neuronal regeneration and differentiation via the BDNF/TrkB signaling pathway: a key target against neurodegenerative diseases?

Mirjana Antonijevic , Patrick Dallemagne , Christophe Rochais
Neural Regeneration Research, 2024, 19 (3), pp.495-496. ⟨10.4103/1673-5374.380896⟩
Article dans une revue hal-04414820 v1
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Development of Pleiotropic TrkB and 5-HT4 Receptor Ligands as Neuroprotective Agents

Mirjana Antonijevic , Despoina Charou , Audrey Davis , Thomas Curel , Maria Valcarcel et al.
Molecules, 2024, 29 (2), pp.515. ⟨10.3390/molecules29020515⟩
Article dans une revue hal-04414817 v1

Synthesis, in vitro and in vivo biological evaluation of novel dual compounds targeting both acetylcholinesterase and serotonergic 5-HT4 receptors with potential interest in the treatment of Alzheimer's disease

Christophe Rochais , Cédric Lecoutey , Julien Lalut , Audrey Davis , Emilie Duval et al.
European Journal of Medicinal Chemistry, 2024, 280, pp.116975. ⟨10.1016/j.ejmech.2024.116975⟩
Article dans une revue hal-04768607 v1
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Synthesis, in vitro and in vivo biological evaluation of novel dual compounds targeting both acetylcholinesterase and serotonergic 5-HT4 receptors with potential interest in the treatment of Alzheimer's disease

Christophe Rochais , Cédric Lecoutey , Julien Lalut , Audrey Davis , Emilie Duval et al.
European Journal of Medicinal Chemistry, 2024, 280, pp.116975. ⟨10.1016/j.ejmech.2024.116975⟩
Article dans une revue hal-04760765 v1
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Studies on the mechanisms of action of MR33317

Joachim Neumann , C. Hesse , S. Yahiaoui , P. Dallemagne , Christophe Rochais et al.
Naunyn-Schmiedeberg's Archives of Pharmacology, 2024, 397 (11), pp.8893-8902. ⟨10.1007/s00210-024-03226-0⟩
Article dans une revue hal-04768605 v1

Synthesis and interest in medicinal chemistry of β-phenylalanine derivatives (β-PAD): an update (2010–2022)

Chloé Rémondin , Serge Mignani , Christophe Rochais , Patrick Dallemagne
Future Medicinal Chemistry, 2024, 16 (11), pp.1147-1162. ⟨10.1080/17568919.2024.2347063⟩
Article dans une revue hal-04627791 v1

Discovery of a pocket network on the domain 5 of the TrkB receptor – A potential new target in the quest for the new ligands

Mirjana Antonijevic , Jana Sopkova-de Oliveira Santos , Patrick Dallemagne , Christophe Rochais
Molecular Informatics, 2024, 43 (8), pp.e202400043. ⟨10.1002/minf.202400043⟩
Article dans une revue hal-04672962 v1
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Dynamic microfluidic single-cell screening identifies pheno-tuning compounds to potentiate tuberculosis therapy

Maxime Mistretta , Mena Cimino , Pascal Campagne , Stevenn Volant , Etienne Kornobis et al.
Nature Communications, 2024, 15 (1), pp.4175. ⟨10.1038/s41467-024-48269-2⟩
Article dans une revue hal-04578611 v1
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C3-Symmetric Ligands in Drug Design: When the Target Controls the Aesthetics of the Drug

Mirjana Antonijevic , Christophe Rochais , Patrick Dallemagne
Molecules, 2023, 28 (2), pp.679. ⟨10.3390/molecules28020679⟩
Article dans une revue hal-03969919 v1
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Conceptual Framework of the Design of Pleiotropic Drugs against Alzheimer’s Disease

Thomas Guiselin , Cédric Lecoutey , Christophe Rochais , Patrick Dallemagne
Pharmaceutics, 2023, 15 (10), pp.2382. ⟨10.3390/pharmaceutics15102382⟩
Article dans une revue hal-04414828 v1
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Biginelli Reaction Synthesis of Novel Multitarget-Directed Ligands with Ca2+ Channel Blocking Ability, Cholinesterase Inhibition, Antioxidant Capacity, and Nrf2 Activation

Rim Malek , Alexey Simakov , Audrey Davis , Maciej Maj , Paul Bernard et al.
Molecules, 2023, 28 (1), pp.71. ⟨10.3390/molecules28010071⟩
Article dans une revue hal-03969932 v1

Advances in prodrug design for Alzheimer’s disease: the state of the art

Valentin Travers--Lesage , Serge Mignani , Patrick Dallemagne , Christophe Rochais
Expert Opinion on Drug Discovery, 2022, 17 (4), pp.325-341. ⟨10.1080/17460441.2022.2031972⟩
Article dans une revue hal-03969939 v1

Aminothiaindanone as an Accessible Scaffold for a Three-Point Chemical Diversity

Pauline Zipfel , Julien Lalut , Jana Sopková-de Oliveira Santos , Christophe Rochais , Patrick Dallemagne
Synthesis: Journal of Synthetic Organic Chemistry, 2021, 53 (20), pp.3799-3814. ⟨10.1055/a-1523-1409⟩
Article dans une revue hal-03969969 v1
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Desirable drug–drug interactions or when a matter of concern becomes a renewed therapeutic strategy

Benjamin Guieu , Jean-Pierre Jourdan , Aurore Dreneau , Nicolas Willand , Christophe Rochais et al.
Drug Discovery Today, 2021, 26 (2), pp.315-328. ⟨10.1016/j.drudis.2020.11.026⟩
Article dans une revue hal-03969988 v1
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First Synthesis of Racemic Trans Propargylamino-Donepezil, a Pleiotrope Agent Able to Both Inhibit AChE and MAO-B, with Potential Interest against Alzheimer’s Disease

Benjamin Guieu , Cedric Lecoutey , Rémi Legay , Audrey Davis , Jana Sopkova de Oliveira Santos et al.
Molecules, 2021, 26 (1), pp.80. ⟨10.3390/molecules26010080⟩
Article dans une revue hal-03969980 v1

Disproportionality analysis in VigiBase as a drug repositioning method for the discovery of potentially useful drugs in Alzheimer's disease

Basile Chrétien , Jean‐pierre Jourdan , Audrey Davis , Sophie Fedrizzi , Ronan Bureau et al.
British Journal of Clinical Pharmacology, 2021, 87 (7), pp.2830-2837. ⟨10.1111/bcp.14690⟩
Article dans une revue hal-03969985 v1

5-HT4R modulators: a patent landscape

Patrick Dallemagne , Christophe Rochais
Pharmaceutical Patent Analyst, 2021, 10 (4), pp.179-181. ⟨10.4155/ppa-2021-0017⟩
Article dans une revue hal-03969965 v1
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Development of Novel Potential Pleiotropic Compounds of Interest in Alzheimer’s Disease Treatment through Rigidification Strategy

Cédric Lecoutey , Rémi Legay , Audrey Davis , Jana Sopková-de Oliveira Santos , Patrick Dallemagne et al.
Molecules, 2021, 26 (9), pp.2536. ⟨10.3390/molecules26092536⟩
Article dans une revue hal-03969972 v1
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Donecopride, a Swiss army knife with potential interest against Alzheimer's disease

Christophe Rochais , Cédric Lecoutey , Katia Hamidouche , Patrizia Giannoni , Florence Gaven et al.
British Journal of Pharmacology, In press, 177 (9), pp.1988-2005. ⟨10.1111/bph.14964⟩
Article dans une revue hal-02428730 v1
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hERG toxicity assessment: Useful guidelines for drug design

Amanda Garrido , Alban Lepailleur , Serge M Mignani , Patrick Dallemagne , Christophe Rochais
European Journal of Medicinal Chemistry, 2020, 195, ⟨10.1016/j.ejmech.2020.112290⟩
Article dans une revue hal-04951714 v1
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Matrix metalloproteinases as new targets in Alzheimer's disease: Opportunities and Challenges

Pauline Zipfel , Christophe Rochais , Kévin Baranger , Santiago Rivera , Patrick Dallemagne
Journal of Medicinal Chemistry, 2020, ⟨10.1021/acs.jmedchem.0c00352⟩
Article dans une revue hal-03461436 v1
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Drug repositioning: a brief overview

Jean-Pierre Jourdan , Ronan Bureau , Christophe Rochais , Patrick Dallemagne
Journal of Pharmacy and Pharmacology, 2020, 72 (9), pp.1145-1151. ⟨10.1111/jphp.13273⟩
Article dans une revue hal-03961788 v1
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hERG toxicity assessment: Useful guidelines for drug design

Amanda Garrido , Alban Lepailleur , Serge M. Mignani , Patrick Dallemagne , Christophe Rochais
European Journal of Medicinal Chemistry, 2020, 195, pp.112290 -. ⟨10.1016/j.ejmech.2020.112290⟩
Article dans une revue hal-03490407 v1
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Pharmacotechnical Development of a Nasal Drug Delivery Composite Nanosystem Intended for Alzheimer’s Disease Treatment

Thomas Adnet , Anne-Claire Groo , Céline Picard , Audrey Davis , Sophie Corvaisier et al.
Pharmaceutics, 2020, 12 (3), pp.251. ⟨10.3390/pharmaceutics12030251⟩
Article dans une revue hal-03969997 v1

Facing the complexity of Alzheimer's disease

Patrick Dallemagne , Christophe Rochais
Future Medicinal Chemistry, 2020, 12 (3), pp.175-177. ⟨10.4155/fmc-2019-0310⟩
Article dans une revue hal-03970000 v1
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Structure-activity relationships of serotonin 5-HT7 receptors ligands: A review

Sangeetha-Laura Thirumaran , Alban Lepailleur , Christophe Rochais
European Journal of Medicinal Chemistry, 2019, 183, pp.111705 -. ⟨10.1016/j.ejmech.2019.111705⟩
Article dans une revue hal-03488662 v1
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26th Annual GP2A Medicinal Chemistry Conference & 32nd Journées Franco-Belges de Pharmacochimie

Patrick Dallemagne , Christophe Rochais , Pascal Marchand , Thierry Besson
Pharmaceuticals, 2019, 12 (2), pp.73. ⟨10.3390/ph12020073⟩
Article dans une revue hal-02330438 v1
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A chemical screen identifies two novel small compounds that alter Arabidopsis thaliana pollen tube growth

Ferdousse Laggoun , Flavien Dardelle , Jérémy Dehors , Denis Falconet , Azeddine Driouich et al.
BMC Plant Biology, 2019, 19, pp.152. ⟨10.1186/s12870-019-1743-9⟩
Article dans une revue hal-02106475 v1
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Novel multi target-directed ligands targeting 5-HT4 receptors with in cellulo antioxidant properties as promising leads in Alzheimer's disease

Caroline Lanthier , Hugo Payan , Irene Liparulo , Bérénice Hatat , Cédric Lecoutey et al.
European Journal of Medicinal Chemistry, 2019, 182, pp.111596. ⟨10.1016/j.ejmech.2019.111596⟩
Article dans une revue hal-02399942 v1

Benzylphenylpyrrolizinones with Anti-amyloid and Radical Scavenging Effects, Potentially Useful in Alzheimer's Disease Treatment

Jean-Pierre Jourdan , Marc Since , Laïla El kihel , Cédric Lecoutey , Sophie Corvaisier et al.
ChemMedChem, 2017, 12 (12), pp.913-916. ⟨10.1002/cmdc.201700102⟩
Article dans une revue hal-02043731 v1

Modulating 5-HT 4 and 5-HT 6 receptors in Alzheimer’s disease treatment

Julien Lalut , Delphine Karila , Patrick Dallemagne , Christophe Rochais
Future Medicinal Chemistry, 2017, 9 (8), pp.781-795. ⟨10.4155/fmc-2017-0031⟩
Article dans une revue hal-02043735 v1

3-(Dipropylamino)-5-hydroxybenzofuro[2,3-f]quinazolin-1(2H)-one (DPA-HBFQ-1) plays an inhibitory role on breast cancer cell growth and progression

Pietro Rizza , Michele Pellegrino , Anna Caruso , Domenico Iacopetta , Maria Stefania Sinicropi et al.
European Journal of Medicinal Chemistry, 2016, 107, pp.275-287. ⟨10.1016/j.ejmech.2015.11.004⟩
Article dans une revue hal-02043777 v1

Design, synthesis, and pharmacological evaluation of multitarget-directed ligands with both serotonergic subtype 4 receptor (5-HT 4 R) partial agonist and 5-HT 6 R antagonist activities, as potential treatment of Alzheimer’s disease

Samir Yahiaoui , Katia Hamidouche , Céline Ballandonne , Audrey Davis , Jana Sopkova-de Oliveira Santos et al.
European Journal of Medicinal Chemistry, 2016, 121, pp.283-293. ⟨10.1016/j.ejmech.2016.05.048⟩
Article dans une revue hal-02043759 v1

Novel benzylidenephenylpyrrolizinones with pleiotropic activities potentially useful in Alzheimer's disease treatment

Jean-Pierre Jourdan , Marc Since , Laïla El Kihel , Cédric Lecoutey , Sophie Corvaisier et al.
European Journal of Medicinal Chemistry, 2016, 114, pp.365-379. ⟨10.1016/j.ejmech.2016.03.023⟩
Article dans une revue hal-02043765 v1

Chronic activation of 5-HT4 receptors or blockade of 5-HT6 receptors improve memory performances

Anne Quiedeville , Michel Boulouard , Katia Hamidouche , Virginie da Silva Costa-Aze , Gerald Nee et al.
Behavioural Brain Research, 2015, 293, pp.10-17. ⟨10.1016/j.bbr.2015.07.020⟩
Article dans une revue hal-02043824 v1

Therapeutic Potential of 5-HT 6 Receptor Agonists

Delphine Karila , Thomas Freret , Valentine Bouet , Michel Boulouard , Patrick Dallemagne et al.
Journal of Medicinal Chemistry, 2015, 58 (20), pp.7901-7912. ⟨10.1021/acs.jmedchem.5b00179⟩
Article dans une revue hal-02043781 v1

Indenopyrazole oxime ethers: Synthesis and β1-adrenergic blocking activity

Tomaso Angelone , Anna Caruso , Christophe Rochais , Angela Caputa , Maria Cerra et al.
European Journal of Medicinal Chemistry, 2015, 92, pp.672-681. ⟨10.1016/j.ejmech.2015.01.037⟩
Article dans une revue hal-01116512 v1

Recent Advances in Phenanthroindolizidine and Phenanthroquinolizidine Derivatives with Anticancer Activities

Maria Fatima Pereira , Christophe Rochais , Patrick Dallemagne
Anti-Cancer Agents in Medicinal Chemistry, 2015, 15 (9), pp.1080-1091. ⟨10.2174/1871520615666150520143600⟩
Article dans une revue hal-02043788 v1
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Design of donecopride, a dual serotonin subtype 4 receptor agonist/acetylcholinesterase inhibitor with potential interest for Alzheimer's disease treatment

Cédric Lecoutey , Damien Hedou , Thomas Freret , Patrizia Giannoni , Florence Gaven et al.
Proceedings of the National Academy of Sciences of the United States of America, 2014, 111 (36), pp.E3825--30. ⟨10.1073/pnas.1410315111⟩
Article dans une revue hal-01800439 v2

MR22388, a novel anti-cancer agent with a strong FLT-3 ITD kinase affinity.

Christophe Rochais , Thierry Cresteil , Vittoria Perri , Marie Jouanne , Aurélien Lesnard et al.
Cancer Letters, 2013, 331 (1), pp.92-8. ⟨10.1016/j.canlet.2012.12.017⟩
Article dans une revue istex hal-00807871 v1

Design, synthesis and biological evaluation of novel indano- and thiaindano-pyrazoles with potential interest for Alzheimer's disease.

David Genest , Christophe Rochais , Cédric Lecoutey , Jana Sopkova-de Oliveira Santos , Céline Ballandonne et al.
MedChemComm, 2013, 4, pp.925-931
Article dans une revue hal-00840942 v1

An unusual boron tribromide-mediated, one-pot bromination/cyclization reaction. Application to the synthesis of a highly strained cyclopenta[1,3]cyclopropa[1,2-b]pyrrolizin-8-one.

Jean-Pierre Jourdan , Christophe Rochais , Rémi Legay , Jana Sopkova-de Oliveira Santos , Patrick Dallemagne
Tetrahedron Letters, 2013, 54 (9), pp.1133-1136
Article dans une revue hal-00821455 v1

Tripentones: A Promising Series of Potent Anti-Cancer Agents.

Christophe Rochais , Sylvain Rault , Patrick Dallemagne
Anti-Cancer Agents in Medicinal Chemistry, 2013, 2, pp.313-343
Article dans une revue hal-00840950 v1

Synergistic effect of acetylcholinesterase inhibition (donepezil) and 5-HT(4) receptor activation (RS67333) on object recognition in mice.

Thomas Freret , Valentine Bouet , Anne Quiedeville , Gérald Nee , Patrick Dallemagne et al.
Behavioural Brain Research, 2012, 230 (1), pp.304-8. ⟨10.1016/j.bbr.2012.02.012⟩
Article dans une revue istex hal-00862757 v1

Synergistic effect of acetylcholinesterase inhibition (donepezil) and 5-HT4 receptor activation (RS67333) on object recognition in mice.

Thomas Freret , Valentine Bouet , Anne Quiedeville , Gérald Nee , Patrick Dallemagne et al.
Behavioural Brain Research, 2012, 230 (1), pp.304-308. ⟨10.1016/j.bbr.2012.02.012⟩
Article dans une revue istex hal-00821461 v1

Synthesis of novel 7-oxo and 7-hydroxy trifluoroallocolchicinoids with cytotoxic effect

Elizabeth Chosson , Francesca Santoro , Christophe Rochais , Jana Sopkova-de Oliveira Santos , Rémi Legay et al.
Bioorganic and Medicinal Chemistry Letters, 2012, 20 (8), pp.2614-2623. ⟨10.1016/j.bmc.2012.02.043⟩
Article dans une revue istex hal-02357753 v1

Synthesis of dual AChE/5-HT4 receptor multi-target directed ligands.

Cédric Lecoutey , Christophe Rochais , David Genest , Sabrina Butt-Gueulle , Céline Ballandonne et al.
MedChemComm, 2012, 3, pp.627-634
Article dans une revue hal-00764795 v1

One-pot synthesis of new aza- and diaza-aminopenanthrenes

Christophe Rochais , Rodrigue Yougnia , Thomas Cailly , Jana Sopkova-de Oliveira Santos , Sylvain Rault et al.
Tetrahedron, 2011, 67 (32), pp.5806-5810. ⟨10.1016/j.tet.2011.05.116⟩
Article dans une revue istex hal-01061754 v1

First and mild synthesis of fluorene-9-malonic acid and some substituted derivatives via the intramolecular hydroarylation of 2-phenylbenzylidenemalonic acids

Elizabeth Chosson , Christophe Rochais , Rémi Legay , Jana Sopkova-de Oliveira Santos , Sylvain Rault et al.
Tetrahedron, 2011, 67 (14), pp.2548-2554. ⟨10.1016/j.tet.2011.02.026⟩
Article dans une revue istex hal-01018072 v1

One-pot synthesis of novel poly-substituted phenanthrenes

Rodrigue Yougnia , Christophe Rochais , Jana Sopkova-de Oliveira Santos , Patrick Dallemagne , Sylvain Rault
Tetrahedron, 2010, 66 (15), pp.2803-2808. ⟨10.1016/j.tet.2010.02.060⟩
Article dans une revue hal-02045958 v1

Intramolecular Cyclisation of β-Aryl-β-Amino Acids in the Design of Novel Heterocyclic Systems with Therapeutic Interest: An Unfailing Source of Diversity

Christophe Rochais , Sylvain Rault , Patrick Dallemagne
Current Medicinal Chemistry, 2010, 17 (35), pp.4342-4369. ⟨10.2174/092986710793361261⟩
Article dans une revue hal-02045949 v1

Virtual Screening Discovery of New Acetylcholinesterase Inhibitors Issued from CERMN Chemical Library

Jana Sopkova-de Oliveira Santos , Aurélien Lesnard , Jean-Hugues Agondanou , Nathalie Dupont , Anne-Marie Godard et al.
Journal of Chemical Information and Modeling, 2010, 50 (3), pp.422-428. ⟨10.1021/ci900491t⟩
Article dans une revue hal-00705935 v1

Hydrogenative desulphurization of thienopyrrolizinones: An easy and selective access to (Z)-phenethylidenepyrrolizinones with in vitro cytotoxic activity

Vittoria Perri , Christophe Rochais , Jana Sopkova-de Oliveira Santos , Rémi Legay , Thierry Cresteil et al.
European Journal of Medicinal Chemistry, 2010, 45 (3), pp.1146-1150. ⟨10.1016/j.ejmech.2009.12.021⟩
Article dans une revue istex hal-02045946 v1

Synthesis, reactivity and biological evaluation of novel halogenated tripentones.

Vittoria Perri , Christophe Rochais , Thierry Cresteil , Patrick Dallemagne , Sylvain Rault
Bioorganic and Medicinal Chemistry, 2009, 17 (22), pp.7783-8. ⟨10.1016/j.bmc.2009.09.027⟩
Article dans une revue istex hal-00433244 v1

Synthesis of new dipyrrolo- and furopyrrolopyrazinones related to tripentones and their biological evaluation as potential kinases (CDKs1-5, GSK-3) inhibitors.

Christophe Rochais , Nghia Vu Duc , Elodie Lescot , Jana Sopkova-de Oliveira Santos , Ronan Bureau et al.
European Journal of Medicinal Chemistry, 2008, epub ahead of print. ⟨10.1016/j.ejmech.2008.05.011⟩
Article dans une revue istex hal-00319802 v1
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29th Annual GP2A Medicinal Chemistry Conference

Jean-Jacques Helesbeux , Laura Carro , Florence Mccarthy , Vânia Moreira , Francesca Giuntini et al.
29th Annual GP2A Medicinal Chemistry Conference, Pharmaceuticals, 14 (12), pp.1278, 2021, ⟨10.3390/ph14121278⟩
Proceedings/Recueil des communications hal-03969961 v1

2,5-Dimethoxytetrahydrofuran, first update

Christophe Rochais , Patrick Dallemagne
John Wiley & Sons, pp.2012, 2012, 9780471936237. ⟨10.1002/047084289X.rd289.pub2⟩
Ouvrages (dictionnaire, encyclopédie) hal-00821463 v1