Mu.Ta.Lig - COST ACTION CA15135

Prof. Christophe ROCHAIS

14 June 2016


General information

Surname: Christophe
Cell phone number with international prefix: +0033687659230
Country: France
Affiliation: Université de Caen Normandie
Gender: F □ M R
Year of the PhD title: 2005
Personal web page:
Previous COST participation: No R Yes


List of 10 selected publications within last 5 years

1.J.-P. Jourdan, M. Since, L. El Kihel, C. Lecoutey, S. Corvaisier, R. Legay, J. Sopkova-de Oliveira Santos, T. Cresteil, A. Malzert-Fréon, C. Rochais,* P. Dallemagne* Novel benzylidenephenylpyrrolizinones with pleiotropic activities potentially useful in Alzheimer’s disease treatment. Eur. J. Med. Chem. 2016, 114, 365-379
2. A. Quiedeville, M. Boulouard, K. Hamidouche, V. Da Silva Costa-Aze, G. Nee, C. Rochais, P. Dallemagne, F. Fabis, T. Freret, V. Bouet, Chronic activation of 5-HT4 receptors or blockade of 5-HT6 receptors improve memory performances, Behav. Brain Res., 2015, 293, 10-17
3. D. Karila, T. Freret, V. Bouet, M. Boulouard, P. Dallemagne*, C. Rochais* Therapeutic potential of 5-HT6 receptor agonists, J. Med. Chem., 2015, 58 (20), 7901–7912
4. C. Rochais*, C. Lecoutey, F. Gaven, P. Giannoni, K. Hamidouche, D. Hedou, E. Dubost, D. Genest, S. Yahiaoui, T. Freret, V. Bouet, F. Dauphin, J. Sopkova de Oliveira Santos, C. Ballandonne, S. Corvaisier, A. Malzert-Fréon, R. Legay, M. Boulouard, S. Claeysen, P. Dallemagne*,Novel Multitarget-Directed Ligands (MTDLs) with Acetylcholinesterase (AChE) Inhibitory and Serotonergic Subtype 4 Receptor (5-HT4R) Agonist Activities As Potential Agents against Alzheimer’s Disease: The Design of Donecopride, J. Med. Chem., 2015, 58 (7), 3172–3187
5. C. Lecoutey, D. Hedou, T. Freret, P. Giannoni, F. Gaven, M. Since, V. Bouet, C. Ballandonne, S. Corvaisier, A. Malzert-Fréon, S. Mignani, T. Cresteil, M. Boulouard, S. Claeysen, C. Rochais*, P. Dallemagne*, Design of donecopride, a dual serotonin subtype 4 receptor agonist/acetylcholinesterase inhibitor with potential interest for Alzheimer’s disease treatment, Proc. Natl. Acad. Sci. USA, 2014, 111(36), E3825–E3830
6. C. Rochais*, T.Cresteil, V.Perri, M.Jouanne, A.Lesnard, S.Rault, P. Dallemagne, MR22388, a Novel Very Specific FLT-3 ITD Kinase Inhibitor, Cancer Lett., 2013, 331, 92-98
7. D. Genest, C. Rochais*, J. Sopkova-de Oliveira Santos, C. Ballandonne, S. Butt-Gueulle, R. Legay, P. Dallemagne, Design, Synthesis and Biological Evaluation of Novel Indano- and Thiaindano-Pyrazoles as Dual Binding Site Acetylcholinesterase Inhibitors Med. Chem.Commun.,2013, 4(6), 925-931
8. C. Lecoutey, C. Rochais, D. Genest, S. Butt-Gueulle, C. Ballandonne, S. Corvaisier, F. Dulin, A. Lepailleur, J. Sopkova-de Oliveira Santos, P. Dallemagne, Synthesis of Dual AChE /5-HT4 Receptors Multi-Target Directed Ligands, Med. Chem. Commun., 2012, 3, 627-634
9. T. Freret, V. Bouet, A. Quiedeville, G. Nee, P. Dallemagne, C. Rochais, M. Boulouard, Synergistic effect of acetylcholinesterase inhibition (donepezil) and 5-HT4 receptor activation (RS67333) on object recognition in mice. A new hope to design a treatment for Alzheimer’s disease, Behav. Brain Res., 2012, 230, 304-308
10. J. Sopkovà-de Oliveira Santos, A. Lesnard, J.-H. Agondanou, N. Dupont, A.-M. Godard, S.Stiebing, C. Rochais, F. Fabis, P. Dallemagne, R. Bureau and S. Rault, Virtual screening discovery of new Acetylcholinesterase inhibitors issued from CERMN chemical library.J. Chem. Inf. Model., 2010,50, 422-428


Main skills and expertise (up to 5)

1.Medicinal chemistry for neurosciences and oncology
2.MultiTarget Directed Ligand development for neurodegenerative disease, including Alzheimer’s disease
3.Medicinal chemistry of serotonergic ligands
4.Medicinal chemistry of Acetylcholinesterase
5.Organic and heterocyclic synthesis


Main equipment/facilities available in the participants’ lab (up to 5)

1.State of the art medicinal chemistry platform
2.Original chemical library (including > 17000 original compounds)
3.Molecular modeling facilities
4.In vitro screening and drugability evaluation platform
5. X-ray diffractometer for monocrystals



Short personal activity proposal for the COST Action CA15135 (max 1000 characters)

We have in our research group in Caen ( over the last five years created an interdisciplinary polypharmacoloy research program which includes expertise in organic, medicinal and analytical chemistry as well as in molecular modeling, data mining and in vitro (AChE, BuChE, 5-HTRs radiobinding) and drugability evaluation (PAMPA, logP…). The program aims at both improving by means of data mining the characterization of pharmacological networks that cause multifactorial pathologies and suggesting innovative therapeutic approaches such as pleiotropic molecules for the treatment of Alzheimer’s disease. This expertise could be proposed to other teams within the frame of the cost action as well as the screening (by us or by partner) of our original chemical library, containing more thant17,000 original compounds. Finally we will organize in July 2016 an international conference on drug design, the RICT, and a satellite meeting could be envisaged for the COST action.


Work Group preference: score from 1 (preferred) to 4 (not preferred)

Work Group of the CA15135 COST Action Score
WG1: Development of new chemical entities 1
WG2: Selection of biological targets and assessment of biological data 3
WG3: Development of chemical databases 4
WG4: Development of Computational methods for multiple ligand design and discovery 2