LCC
Overview
Our work, combining chemistry and biology, is based on different pharmacological approaches such as the understanding of:
1) the mechanisms of resistance of pathogens to drugs, and
2) the mode of action of molecules of therapeutic interest.
These studies lead to the design, synthesis, evaluation and mechanistic studies of drug candidates for the treatment of pathologies in which transition metals are involved such as malaria, Alzheimer’s disease, etc… Our team is also labelled Inserm (ERL 1289, MAAP).
Members of the team
No Results Found
Research topics
Mechanisms of Plasmodium resistance and therapeutic targets
Markers of resistance selection
Mechanochemical approaches for the synthesis of antimalarial molecules
Alzheimer disease
Team news
Lawsone featured in ACS Molecule of the Week
A study by the LCC (Michel Baltas, Anne Robert et al.) and the University of Tartu (Estonia) cited in ‘ACS Molecule of the Week’.
Unprecedented linear products by a mechanochemically activated Biginelli reaction using lawsone
Published in “RCS Mechanochemistry”
This study has been the subject of a scientific update from the CNRS Chemistry Institute.
2022 Team V Poster
Keywords: antimalarial molecules, Plasmodium falciparum
Publications
2024
In vitro evaluation of ganaplacide/lumefantrine combination against Plasmodium falciparum in a context of artemisinin resistance
Manaranche J., Laurent M., Tressieres R., Nguyen M., Salim M., Ouji M., Reyser T., Egwu C. O., Robert A., Augereau J.-M., Benoit-Vical F., Paloque L.
Journal of Antimicrobial Chemotherapy 2024, 79(11), 2877–2886.
https://doi.org/10.1093/jac/dkae300
https://hal.science/hal-04725400
In artemisinin-resistant falciparum malaria parasites, mitochondrial metabolic pathways are essential for survival but not those of apicoplast
Ouji M., Reyser T., Yamaryo-Botté Y., Nguyen M., Rengel D., Dutreuil A., Marcellin M., Burlet-Schiltz O., Augereau J.-M., Riscoe M. K., Paloque L., Botté C., Benoit-Vical F.
International Journal for Parasitology: Drugs and Drug Resistance 2024, 26, 100565/1-15.
https://doi.org/10.1016/j.ijpddr.2024.100565
https://hal.science/hal-04725507
Peptide-alkoxyamine drugs: an innovative approach to fight schistosomiasis: “digging their graves with their forks”
Embo-Ibouanga A. W., Nguyen M., Joly J.-P., Coustets M., Augereau J.-M., Paloque L., Vanthuyne N., Bikanga R., Robert A., Benoit-Vical F., Audran G., Mellet P., Boissier J., Marque S. R. A.
Pathogens 2024, 13(6), 482/1-16.
https://doi.org/10.3390/pathogens13060482
https://hal.science/hal-04632259
Characterization of antimalarial activity of artemisinin-based hybrid drugs
Costa Quadros H., Herrmann L., Manaranche J., Paloque L., Borges-Silva M. C., Akpeko Dziwornu G., D’Alessandro S., Chibale K., Basilico N., Benoit-Vical F., Tsogoeva S. B., Rodrigo Moreira D. M.
Antimicrobial Agents and Chemotherapy 2024, 68(7), e00143-24/1-22.
https://doi.org/10.1128/aac.00143-24
https://hal.science/hal-04631752
Copper selective 8-aminoquinoline based tetradentate chelators as anticancer agents
Guan Y., Nguyen M., Robert A., Liu Y., Meunier B.
RSC Medicinal Chemistry 2024, 15(9), 3048-3056.
http://dx.doi.org/10.1039/D4MD00171K
https://hal.science/hal-04606276
Unprecedented linear products by a mechanochemically activated Biginelli reaction using lawsone
Koumpoura C. L., Vendier L., Bijani C., Robert A., Carbonnière P., Sotiropoulos J.-M., Baltas M.
RSC Mechanochemistry 2024, 1(2), 167-175.
http://dx.doi.org/10.1039/D3MR00032J
https://hal.science/hal-04550806
The synthesis of 2′-hydroxychalcones under ball mill conditions and their biological activities
Abid I., Moslah W., Cojean S., Imbert N., Loiseau P. M., Chamayou A., Srairi-Abid N., Calvet R., Baltas M.
Molecules 2024, 29(8), 1819/1-20.
https://doi.org/10.3390/molecules29081819
https://hal.science/hal-04550832
Hybrid peptide-alkoxyamine drugs: A strategy for the development of a new family of antiplasmodial drugs
Embo-Ibouanga A. W., Nguyen M., Paloque L., Coustets M., Joly J.-P., Augereau J.-M., Vanthuyne N., Bikanga R., Coquin N., Robert A., Audran G., Boissier J., Mellet P., Benoit-Vical F., Marque S. R. A.
Molecules 2024, 29 (6), 1397/1-19.
https://doi.org/10.3390/molecules29061397
https://hal.science/hal-04515160
Epigenetic regulation as a therapeutic target in the malaria parasite Plasmodium falciparum
Reyser T., Paloque L., Augereau J.-M., Di Stefano L., Benoit-Vical F.
Malaria Journal 2024, 23 (1), 44/1-18.
https://doi.org/10.1186/s12936-024-04855-9
https://hal.science/hal-04502290
Synthesis of novel artemisinin, ciprofloxacin, and norfloxacin hybrids with potent antiplasmodial activity
Vamvoukaki G., Antoniou A. I., Baltas M., Mouray E., Charneau S., Grellier P., Athanassopoulos C. M.
Antibiotics 2024, 13 (2), 142/1-22.
https://doi.org/10.3390/antibiotics13020142
https://hal.science/hal-04509679
2023
The specific copper(II) chelator TDMQ20 is efficient for the treatment of Wilson’s disease in mice
Zhu Y., Tang Y., Huang L., Nguyen M., Liu Y., Robert A., Meunier B.
Pharmaceutics 2023, 15(12), 2719/1-15.
https://doi.org/10.3390/pharmaceutics15122719
https://hal.science/hal-04322010
Epidrugs as promising tools to eliminate Plasmodium falciparum artemisinin-resistant and quiescent parasites
Reyser T., Paloque L., Nguyen M., Augereau J.-M., Fuchter M. J., Lopez M. J., Arimondo P. B., Hassell-Hart S., Spencer J., Di Stefano L., Benoit-Vical F.
Pharmaceutics 2023, 15(10), 2440/1-15.
https://doi.org/10.3390/pharmaceutics15102440
https://hal.science/hal-04269105
Design, synthesis and evaluation of novel pyrimidinylaminothiophene derivatives as FGFR1 inhibitors against human glioblastoma multiforme
Li Y.-L., Yan L.-J., Chen H.-X., Ruan B.-K., Dao P., Du Z.-Y., Dong C.-Z., Meunier B.
European Journal of Medicinal Chemistry 2023, 260, 115764/1-13.
https://doi.org/10.1016/j.ejmech.2023.115764
https://hal.science/hal-04209922
Hybrid molecules based on an emodin scaffold. Synthesis and activity against SARS-CoV-2 and Plasmodium
Li Y., Touret F., de Lamballerie X., Nguyen M., Laurent M., Benoit-Vical F., Robert A., Liu Y., Meunier B.
Organic & Biomolecular Chemistry 2023, 21(36), 7382-7394.
http://dx.doi.org/10.1039/D3OB01122D
https://hal.science/hal-04201757
Mechanochemical studies on coupling of hydrazines and hydrazine amides with phenolic and furanyl aldehydes-hydrazones with antileishmanial and antibacterial activities
Kapusterynska A., Bijani C., Paliwoda D., Vendier L., Bourdon V., Imbert N., Cojean S., Loiseau P. M., Recchia D., Scoffone V. C., Degiacomi G., Akhir A., Saxena D., Chopra S., Lubenets V., Baltas M.
Molecules 2023, 28(13), 5284/1-26.
https://doi.org/10.3390/molecules28135284
https://hal.science/hal-04157067
Oxidation of TDMQ20, a specific copper Chelator as potential drug against Alzheimer’s disease
Nguyen M., Li Y., Robert A., Liu Y., Meunier B.
ChemistrySelect 2023, 8(8), e202204877/1-8.
https://doi.org/10.1002/slct.202204877
https://hal.science/hal-04007798
2022
Distribution in rat blood and brain of TDMQ20, a copper chelator designed as a drug-candidate for Alzheimer’s disease
Huang L., Zeng Y., Li Y., Zhu Y., He Y., Liu Y., Robert A., Meunier B.
Pharmaceutics 2022, 14(12), 2691/1-13.
https://doi.org/10.3390/pharmaceutics14122691
https://hal.science/hal-03985553
Proteomics evidence of the role of TDMQ20 in the cholinergic system and synaptic transmission in a mouse model of Alzheimer’s disease
Sun F., Zhao J., Zhang H., Shi Q., Liu Y., Robert A., Liu Q., Meunier B.
ACS Chemical Neuroscience 2022, 13(21), 3093–3107.
https://doi.org/10.1021/acschemneuro.2c00455
https://hal.archives-ouvertes.fr/hal-03826219
Design of anti-infectious agents from lawsone in a three-component reaction with aldehydes and isocyanides
Koumpoura C. L., Nguyen M., Bijani C., Vendier L., Salina E. G., Buroni S., Degiacomi G., Cojean S., Loiseau P. M., Benoit-Vical F., García-Sosa A. T., Robert A., Baltas M.
ACS Omega 2022, 7(40), 35635-35655.
https://doi.org/10.1021/acsomega.2c03421
https://hal.archives-ouvertes.fr/hal-03818601
In vitro and in silico antimalarial evaluation of FM-AZ, a new artemisinin derivative
Tsamesidis I., Mousavizadeh F., Egwu C. O., Amanatidou D., Pantaleo A., Benoit-Vical F., Reybier K., Giannis A.
Medicines 2022, 9(2), 8/1-12.
https://doi.org/10.3390/medicines9020008
https://hal.archives-ouvertes.fr/hal-03660647
How to define a nanozyme
Robert A., Meunier B.
ACS Nano 2022, 16(5), 6956-6959.
https://doi.org/10.1021/acsnano.2c02966
https://hal.archives-ouvertes.fr/hal-03681945
Mutation in the Plasmodium falciparum BTB/POZ domain of K13 protein confers artemisinin resistance
Paloque L., Coppée R., Stokes B. H., Gnädig N. F., Niaré K., Augereau J.-M., Fidock D. A., Clain J., Benoit-Vical F.
Antimicrobial Agents and Chemotherapy 2022, 66(1), e01320-21.
https://doi.org/10.1128/AAC.01320-21
https://hal.archives-ouvertes.fr/hal-03561782
X-Ray diffraction structure of Cu(II) and Zn(II) complexes of 8-aminoquinoline derivatives (TDMQ), related to the activity of these chelators as potential drugs against Alzheimer’s disease
Li Y., Nguyen M., Vendier L., Robert A., Liu Y., Meunier B.
Journal of Molecular Structure 2022, 1251, 132078/1-6.
https://doi.org/10.1016/j.molstruc.2021.132078
https://hal.archives-ouvertes.fr/hal-03509314
Synthesis and antimalarial activities of new hybrid Atokel molecules
Li Y., Loureiro A., Nguyen M., Laurent M., Bijani C., Benoit-Vical F., Robert A., Liu Y., Meunier B.
ChemistryOpen 2022, 11(5), e202200064/1-20.
https://doi.org/10.1002/open.202200064
https://hal.archives-ouvertes.fr/hal-03681793
Resistance to artemisinin in falciparum malaria parasites: A redox-mediated phenomenon
Egwu C. O., Pério P., Augereau J.-M., Tsamesidis I., Benoit-Vical F., Reybier K.
Free Radical Biology and Medicine 2022, 179, 317-327.
https://doi.org/10.1016/j.freeradbiomed.2021.08.016
https://hal.archives-ouvertes.fr/hal-03561900
2021
TDMQ20, a specific copper chelator, reduces memory impairments in Alzheimer’s disease mouse models
Zhao J., Shi Q., Tian H., Li Y., Liu Y., Xu Z., Robert A., Liu Q., Meunier B.
ACS Chemical Neuroscience 2021, 12(1), 140-149.
https://doi.org/10.1021/acschemneuro.0c00621
https://hal.archives-ouvertes.fr/hal-03079460
Novel molecule combinations and corresponding hybrids targeting artemisinin-resistant Plasmodium falciparum parasites
Ouji M., Nguyen M., Mustière R., Jimenez T., Augereau J.-M., Benoit-Vical F., Deraeve C.
Bioorganic & Medicinal Chemistry Letters 2021, 39, 127884/1-6.
https://doi.org/10.1016/j.bmcl.2021.127884
https://hal.archives-ouvertes.fr/hal-03170976
Antimalarial inhibitors targeting epigenetics or mitochondria in Plasmodium falciparum: Recent survey upon synthesis and biological evaluation of potential drugs against malaria
Koumpoura C. L., Robert A., Athanassopoulos C. M., Baltas M.
Molecules 2021, 26(18), 5711/1-34.
https://doi.org/10.3390/molecules26185711
https://hal.archives-ouvertes.fr/hal-03366266
Elucidation of the Diels-Alder reaction kinetics between diphenylfulvene and maleimide by mechanochemistry and in solution
Gonnet L., Chamayou A., André-Barrès C., Micheau J.-C., Guidetti B., Sato T., Baron M., Baltas M., Calvet R.
ACS Sustainable Chemistry & Engineering 2021, 9(12), 4453-4462.
https://doi.org/10.1021/acssuschemeng.0c08314
https://hal.archives-ouvertes.fr/hal-03197711
Synthesis of biologically relevant 1,2,3- and 1,3,4-triazoles: From classical pathway to green chemistry
Gonnet L., Baron M., Baltas M.
Molecules 2021, 26(18), 5667/1-27.
https://doi.org/10.3390/molecules26185667
https://hal.archives-ouvertes.fr/hal-03360993
Superoxide: A major role in the mechanism of action of essential antimalarial drugs
Egwu C. O., Tsamesidis I., Pério P., Augereau J.-M., Benoit-Vical F., Reybier K.
Free Radical Biology and Medicine 2021, 167, 271-275.
https://doi.org/10.1016/j.freeradbiomed.2021.03.001
https://hal.archives-ouvertes.fr/hal-03203905
Reactive oxygen species as the brainbox in malaria treatment
Egwu C. O., Augereau J.-M., Reybier K., Benoit-Vical F.
Antioxidants 2021, 10(12), 1872/1-20.
https://doi.org/10.3390/antiox10121872
https://hal.archives-ouvertes.fr/hal-03542736
A new thienopyrimidinone chemotype shows multistage activity against Plasmodium falciparum, including artemisinin-resistant parasites
Bosson-Vanga H., Primas N., Franetich J.-F., Lavazec C., Gomez L., Ashraf K., Tefit M., Soulard V., Dereuddre-Bosquet N., Le Grand R., Donnette M., Mustière R., Amanzougaghene N., Tajeri S., Suzanne P., Malzert-Fréon A., Rault S., Vanelle P., Hutter S., Cohen A., Snounou G., Roques P., Azas N., Lagardère P., Lisowski V., Masurier N., Nguyen M., Paloque L., Benoit-Vical F., Verhaeghe P., Mazier D., Muralidharan V.
Microbiology Spectrum 2021, 9(2), e00274-21/1-19.
https://doi.org/10.1128/Spectrum.00274-21
https://hal.archives-ouvertes.fr/hal-03363796
2-phenoxy-3-trichloromethylquinoxalines are antiplasmodial aerivatives with activity against the apicoplast of Plasmodium falciparum
Amrane D., Arnold C.-S., Hutter S., Sanz-Serrano J., Collia M., Azqueta A., Paloque L., Cohen A., Amanzougaghene N., Tajeri S., Franetich J.-F., Mazier D., Benoit-Vical F., Verhaeghe P., Azas N., Vanelle P., Botté C., Primas N.
Pharmaceuticals 2021, 14(8), 724/1-24.
https://doi.org/10.3390/ph14080724
https://hal.archives-ouvertes.fr/hal-03323862
“Nanozymes” without catalytic activity should be renamed
[Unpublished work], 2021
Nguyen M., Robert A., Meunier B.
https://hal.archives-ouvertes.fr/hal-03290323
Partnerships
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Alumnae
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Youzhi Li (PhD 2019-2022): post-doc position, Hong-Kong
Chinedu Egwu (PhD 2018-2021): Professor assistant, FUNAI University, Nigeria
Thibaud Reyser (PhD 2017-2020): Technical Service Scientist, Merck KGaA
Manel Ouji (PhD 2017-2020): Medical Information Officer, Pfizer
Sokhna Keita Alassane (PhD 2013-2016)
Arba Pramundita Ramadani (PhD 2013-2017): Professor Assistant, Department of Pharmacy Yogyakarta, Indonesia
Useful links
Click here to view the links
- https://www.cnrs.fr/fr/alzheimer-reguler-le-cuivre-dans-le-cerveau-stoppe-les-pertes-de-memoire-chez-la-souris , décembre 2020, communiqué de presse CNRS
- https://www.cnrs.fr/sites/default/files/press_info/2018-10/CPCNRS_Magnétite_Alzheimer_FRWeb.pdf, 10 octobre 2018, communiqué de presse CNRS.
- https://presse.inserm.fr/mercredi-25-avril-2018-journee-mondiale-de-lutte-contre-le-paludisme/31163/ , avril 2018, communiqué de presse Inserm
- https://presse.inserm.fr/lundi-25-avril-2016-journee-mondiale-de-lutte-contre-le-paludisme/23644/ , avril 2016, communiqué de presse Inserm
- https://presse.inserm.fr/paludisme-la-multi-resistance-aux-traitements-devient-plus-alarmante-que-jamais/20674/, septembre 2015, communiqué de presse Inserm
- https://presse.inserm.fr/comment-le-parasite-responsable-des-formes-graves-de-paludisme-resiste-a-un-antipaludique-majeur/16967/, avril 2010, communiqué de presse Inserm
LCC
Laboratoire de chimie de coordination du CNRS
205 route de Narbonne, BP 44099
31077 Toulouse cedex 4
France