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SAID EL KAZZOULI

El Kazzouli Saïd

Ecole EUROMED d’ingénieurs BiomedTech

s.elkazzouli@ueuromed.org

2004: Ph.D. in Organic Chemistry
University of Orleans, Institute of Organic and Analytical Chemistry, Orleans, France. Supervisor: Professor Gérald Guillaumet from the University of Orleans in collaboration with Professor Abderrahim Mouaddib from the University of Cadi Ayyad. Dissertation Title: "Solid support synthesis of various heterocycles from a common synthon. Development and pharmacological evaluation of imidazo[1,2-a]pyridine derivatives as melatonin analogues", Expertise: multi-step synthesis, imidazo[1,2- a]pyridines, melatonin analogues, palladium and copper–catalyzed reactions, solid support synthesis, microwave synthesis.
2000: M.S. in Organic Chemistry
Universities of Orleans, Paris V and Paris XI
Thesis Title: "Support solid synthesis of large C-terminal peptide aldehyde: application to chemoselective ligation". Expertise: solid phase synthesis, peptide chemistry. Centre National de la Recherche Scientifique (CNRS), Centre de Biophysique Moléculaire, Orleans, France. Supervisor: Agnès Delmas, Ph.D.

 

Medicinal chemistry
Synthetic methodologies, 
Green chemistry, 
Macromolecules « dendrimers and dendrons » for drug delivery and MRI
 

2013 to Present:    Euro-Mediterranean University of Fes (UEMF), Morocco. Design and synthesis of   bioactive   molecules,   drugs   delivery   by   macromolecules,   environmental chemistry, green chemistry, phosphate forth flotation and catalysis.
2009-2013:   Institute of Nanomaterials and Nanotechnology, Moroccan Foundation for Advanced Sciences, Innovations and Research (MAScIR), Rabat, Morocco. Design and synthesis of bioactive molecules, drugs delivery by dendrimers, phosphate forth flotation, homogenous catalysis.
2006-2009:  National Institutes of Health (NIH), National Cancer Institute (NCI), Frederick, Maryland, Centre for Cancer Research, Laboratory of Medicinal Chemistry, USA. 
Postdoctoral Fellow (IRTA Fellow): Rational drug design and multi-step synthesis of antitumor agents, purification and characterization of biologically active diacylglycerol-lactones (DAG-lactones). Expertise: solid phase synthesis, parallel synthesis, combinatorial chemistry, diacylglycerol-lactones (DAG-lactones), protein kinase C (PKC), C1-domains.
2004-2006: University of Orleans, Institute of Organic and Analytical Chemistry, Orleans, France.
2005-2006: Postdoctoral Fellow in Heterocyclic Chemistry: Synthesis of herbicide, Expertise: indole chemistry, anionic reactions, in collaboration with Syngenta, Basel, Switzerland.
2005: Postdoctoral Fellow in Nucleosides Chemistry: Synthesis of new antiviral drugs, Expertise: nucleosides chemistry, palladium–catalyzed reactions, solid support synthesis, microwave synthesis. France
2004:  Postdoctoral  Fellow in Heterocyclic Chemistry: Synthesis of new pyrimido[4,5-b][1,4]oxazines, Expertise: pyrimido[4,5-b][1,4]oxazines, palladium-catalyzed N- arylation, microwave synthesis. France.

 

Palladium-catalyzed regioselective C−H arylation of 4-azaindazole at C3, C5 and C7 positions. Faarasse, S.; El Kazzouli, S.; Bourg, S.;  Aci-Sèche, S.; Bonnet, P.; Suzenet, F.; Guillaumet, G. Angew. Chem. Int. Ed. 2020, submitted.
Design, synthesis and biological evaluation of ethacrynic acid derivatives bearing sulfonamides as potent anti-cancer agents. El Abbouchi, A.; El Brahmi, N.; Hiebel, M-A.; Bignon, J.; Guillaumet, G.; Suzenet, F.; El Kazzouli, S. Bioorganic and Medicinal Chemistry Letters, 2020, under review.
“On water” palladium catalyzed direct arylation of 1H-indazole and 1H-7-azaindazole. Gambouz, K.; El Abbouchi, A.; Nassiri, S.; Suzenet, F.; Bousmina, M.; Akssira, M.; Guillaumet, G.; El Kazzouli, S. Molecules, 2020, under review.
Palladium-catalyzed oxidative arylation of 1H-indazoles with arenes. Gambouz, K.; El Abbouchi, A.; Akssira, M.; Guillaumet, G.; El Kazzouli, S. Eur. J. Org. Chem. 2020, Accepted.
Direct arylation and Suzuki-Miyaura coupling of imidazo[1,2-a]pyridines catalyzed by (SIPr)Pd(allyl)Cl complex under microwave-irradiation. El Abbouchi, A.; Koubachi, J.; El Brahmi, N.; El Kazzouli. S. Med J. Chem. 2019, 9, 347. 
Unusual rearrangement of imidazo[1,5-a]imidazoles and imidazo[1,2-b]pyrazoles into imidazo[1,5-a]pyrimidines and pyrazolo[1,5-a]pyrimidines, Gambouz, K.; Loubidi, M.; Tber, Z.; Driowy, M.; Allouchi, H.; El Kazzouli, S. Akssira, M.; Guillaumet, G. RSC Advances, 2019, 9, 29051. 
Oxidative alkenylation of fused bicyclic heterocycles. Koubachi, J.; El Brahmi, N.; Guillaumet, G.; El Kazzouli, S. Eur. J. Org. Chem. 2019, 2568. 
Exploration of biomedical dendrimer space based on in-vitro physicochemical parameters: key factor analysis (Part 1). Mignani, S.; Rodrigues, J.; Roy, R.; Shi, X.; Cenã, V.; El Kazzouli, S.; Majoral. J-P. Drug Discov. Today, 2019, 24, 1176. 
Exploration of biomedical dendrimer space based on in-vitro physicochemical parameters: key factor analysis (Part 2). Mignani, S.; Rodrigues, J.; Roy, R.; Shi, X.; Cenã, V.; El Kazzouli, S.; Majoral. J-P. Drug Discov. Today, 2019, 24, 1184. 
Palladium-catalyzed C3 arylations of 1H and 2H pyrazolo[4,3-b]pyridines on water: One pot direct C3-arylations of 1H and 2H series. Faarasse, S.; El Kazzouli, S.; Suzenet, F.; Guillaumet, G., J. Org. Chem. 2018, 83, 12847-12854.
Synthesis and characterization of new organophilic clay. Preparation of polystyrene/clay nanocomposite, Ben-Yahia, A.; El Kazzouli, S.; Essassi, E.M.; Bousmina, M.M. Scientific Study and Research: Chemistry and Chemical Engineering, Biotechnology, Food Industry, 2018, 19, 193.
On Water” Direct C-3 Arylation of 2H-Pyrazolo[3,4-b]pyridines, Faarasse, S. El Kazzouli, S.; Naas, M.; Jouha, J.; Suzenet, F.; Guillaumet, G., J. Org. Chem. 2017, 82, 12300. 
Original Multivalent Gold(III) and Dual Gold(III)–Copper(II) Conjugated Phosphorus Dendrimers as Potent Antitumoral and Antimicrobial Agents, Mignani, S.; El Brahmi, N.; El Kazzouli, S.; Laurent, R.; Ladeira, S.; Caminade, A-M.; Pedziwiatr-Werbicka, E.; Szewczyk, E. M.; Bryszewska, M.; Bousmina, M.; Cresteil, T.; Majoral, J-P. Molecular Pharmaceutics. 2017, 14, 4087. 
Anticancer copper(II) phosphorus dendrimers are potent proapoptotic Bax activators. Mignani, S. El Brahmi, N.; Eloy, L.; Poupon, J.; Nicolas, V.; Steinmetz, A.; El Kazzouli, S.; Bousmina, M. ; Blanchard-Desce, M.; Caminade, A-M.; Majoral, J-P.; Cresteil, T. Eur. J. Med. Chem. 2017, 132, 142. 
Symmetrical and unsymmetrical incorporation of active biological monomers on the surface of phosphorus dendrimers. El Brahmi, N.; El Kazzouli, S.; Mignani, S.; Laurent. R.; Ladeira. S.; Caminade, A-M.; Bousmina, M.; Majoral, J-P. Tetrahedron. 2017, 73, 1331. 
A  novel  class  of  ethacrynic  acid  derivatives  as  promising  drug-like  potent  generation  of anticancer agents with established mechanism of action. Mignani, S. El Brahmi, N. El Kazzouli, S.: Eloy, L.; Courilleau, D.; Caron, J. S. Bousmina, M. Caminade, A-M. Cresteil, T. Majoral, J-P. Eur. J. Med. Chem. 2016, 122, 656. 
Functionalization  of  Indazoles  by  Means  of  Transition  Metal-Catalyzed  Cross-Coupling Reactions. El Kazzouli, S.; Guillaumet, G., Tetrahedron. 2016, 72, 6711. 
Synthesis and  characterization  of  nanostructured  palladium  perovskites:  Evaluation  of  their catalytic activity in cross-coupling chemistry, Essoumhi, A. Solhy, A. El Kazzouli, S. J. Mater. Environ. Sci. 2016, 7, 1080. 
Palladium-catalyzed oxidative direct C3- and C7-alkenylations of indazoles: Application to the synthesis of Gamendazole. Naas, M. El Kazzouli, S.; Essassi, EM. Bousmina, M.; Guillaumet, G. Org. Lett. 2015, 17, 4320. 
Advances in direct C-H arylation of 5,5, 6,5 and 6,6- fusedheterocycles containing heteroatoms (N, O, S). El Kazzouli, S.; Koubachi, J.; El Brahmi, N.; Guillaumet, G. RSC Advances, 2015, 7, 3915. 
Investigations in dendrimer space reveal solid and liquid tumor growth-inhibition by original phosphorus-based dendrimers and corresponding monomers and dendrons with ethacrynic acid motifs. El Brahmi, N.; Mignani, S.; Caron, J.; El Kazzouli, S.; Bousmina, M.; Caminade, A- M.; Cresteil, T.;  Majoral, J-P. Nanoscale, 2015, 7, 3915. 
Palladium-catalyzed direct C7-arylation of substituted indazoles. Naas, M.; El Kazzouli, S.; Essassi, E. M.; Bousmina, M.; Guillaumet, G. J. Org. Chem. 2014. 79, 7286. 
Ceria-supported copper nanoparticles: A highly efficient and recyclable catalyst for N-arylation of indole. Amadine, O.; Maati, H.; Abdelouhadi, K.; Fihri, A.; El Kazzouli, S.; Len, C.; El Bouari, A.; Solhy. A. Journal of Molecular Catalysis A: Chemical, 2014, 395, 409. 
Functionalization of imidazo[1,2-a]pyridines by means of metal-catalyzed cross-coupling reactions – A review. Koubachi, J.; El Kazzouli, S.; Bousmina, M.; Guillaumet, G. Eur. J. Org. Chem. 2014, 24, 5119. 
Review  on  palladium-containing  perovskites:  Synthesis,  physico-chemical  properties  and applications  in  catalysis.  Essoumhi,  A.;  El  Kazzouli,  S.;  Bousmina,  M.  J.  Nanosci. Nanotechnol. 2014, 14, 2012. 
Dendrimer Space Exploration: Inhibition of protein-protein interactions for the next generation of pharmaceuticals. Mignani, S.; El Kazzouli, S.; Bousmina, M.; Majoral, J-P. Chem. Rev. 2014, 114, 1327. 
Dendrimer space concept for innovative nanomedicine: a futuristic vision in medicinal chemistry.  Mignani,  S.;  El  Kazzouli,  M.;  Bousmina,  M.;  Majoral,  Progress  in  Polymer Science, 2013, 38, 993. 
Original  multivalent  copper(II)-conjugated  phosphorus-dendrimers  and  corresponding mononuclear copper(II) complexes with anti-tumoral activities. El Brahmi, N. El Kazzouli, S. Mignani, S. Essassi, E. Aubert, G. Laurent, R. Caminade, A-M. Bousmina, M. Cresteil, T. Majoral, J-P. Molecular Pharmaceutics, 2013, 10, 1459. 
Expand classical drug administration ways by emerging routes using dendrimer drug delivery systems: a concise overview. Mignani, S.; El Kazzouli, M.; Bousmina, M.; Majoral, J-P. Advanced Drug Delivery Reviews, 2013, 65, 1316. 
Copper in dendrimer’s synthesis and applications of copper dendrimer systems in catalysis: a concise overview. El Brahmi N.; El Kazzouli, M.; Mignani, S.; Bousmina, M.; Majoral, J-P. Tetrahedron, 2013, 69, 3103. 
Microwave-assisted Suzuki-Miyaura cross-coupling of free (NH) 3-bromoindazoles. Benyahia, A.; Naas, M.; El Brahmi, N.; El Kazzouli, S.; Essassi, EM. Majoral, J-P. Guillaumet, G. Current Org. Chem. 2013, 17, 304. 

Patent.

Activités antitumorales d’une nouvelle famille de dérivés de l’acide ethacrynique,
N° de dépôt: 44038, 29/11/2018. Submitted to PCT, Int. Appl. In 2019.
El Kazzouli S.; Abdelmajid, Z.; El Brahmi N.; El Abbouchi A.; Boujdi K.; Bousmina M.; Ait Mouse H.; Tilaoui M. 
 

General chemistry
Organic chemistry
Analytical chemistry
Synthesis, characterization and applications of organic macromolecules