A5071896697- Meningioma and schwannoma management
- Research on Leishmaniasis Studies
- Trypanosoma species research and implications
- Synthesis and Biological Evaluation
- Glioma Diagnosis and Treatment
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Malaria Research and Control
- Synthesis and biological activity
- Neurofibromatosis and Schwannoma Cases
- Neuroendocrine Tumor Research Advances
- Synthesis and Characterization of Heterocyclic Compounds
- HIV/AIDS drug development and treatment
- Computational Drug Discovery Methods
- Quinazolinone synthesis and applications
- Chemical Synthesis and Analysis
- Head and Neck Surgical Oncology
- Phenothiazines and Benzothiazines Synthesis and Activities
- Multicomponent Synthesis of Heterocycles
- Neuroblastoma Research and Treatments
- Microwave-Assisted Synthesis and Applications
- Insect Pest Control Strategies
- Catalytic Cross-Coupling Reactions
- Mosquito-borne diseases and control
- Sulfur-Based Synthesis Techniques
Aix-Marseille Université
2013-2024
Laboratoire de Physique Théorique de la Matière Condensée
2022-2024
Inserm
2023-2024
Méditerranée Infection Foundation
2018-2023
Institut de Recherche pour le Développement
2014-2023
Assistance Publique Hôpitaux de Marseille
2021-2023
Hôpital de la Timone
2020
Génétique et Immunologie des Maladies Parasitaires
2012-2018
Université de Montpellier
2014
Institut de Chimie Radicalaire
2010-2012
Aggressive meningiomas that progress after surgery/radiotherapy represent an unmet medical need. Strong and constant expression of SSTR2A receptors activation the Pi3K/Akt/mTOR pathway have been demonstrated in meningiomas. The combination everolimus, mTOR inhibitor, octreotide, a somatostatin agonist, has shown additive antitumor effect vitro. phase II CEVOREM trial investigated efficacy this on recurrent meningiomas.Patients with documented tumor progression ineligible for further were...
Novel series of bis- and tris-pyrrolo[1,2-a]quinoxaline derivatives 1 were synthesized tested for in vitro activity upon the intraerythrocytic stage W2 3D7 Plasmodium falciparum strains. Biological results showed good antimalarial with IC50 μM range. In attempting to investigate large broad-spectrum antiprotozoal activities these new derivatives, their properties toward Leishmania donovani also investigated revealed selective antiplasmodial profile. parallel, cytotoxicity molecules was...
Twenty nine original 3-nitroimidazo[1,2-a]pyridine derivatives, bearing a phenylthio (or benzylthio) moiety at position 8 of the scaffold, were synthesized. In vitro evaluation highlighted compound 5 as an antiparasitic hit molecule displaying low cytotoxicity for human HepG2 cell line (CC50 > 100 μM) alongside good antileishmanial activities (IC50 = 1–2.1 against L. donovani, infantum, and major; antitrypanosomal 1.3–2.2 T. brucei cruzi, in comparison to several reference drugs such...
A new simple, rapid and high yielding synthesis of various 5-substituted thiazoles by Suzuki–Miyaura cross-coupling reaction is described using microwave irradiation in aqueous medium without organic co-solvent the presence tetrabutylammonium bromide.
Background: We prepared a novel series of enantiopure mefloquine analogues with pyrrolo[ 1,2-a]quinoxaline core in order to fight Plasmodium falciparum resistant strain. Objectives: To observe the influence pyrrolo[1,2-a]quinoxaline versus quinoline on antimalarial activity. Method: Four aminoalcoholpyrrolo[1,2-a]quinoxalines 2 were synthetized via Sharpless asymmetric dihydroxylation reaction eight steps. Their activity was evaluated two strains 3D7 and W2 SYBR Green I fluorescence-based...
A series of new 2,9-bis[(substituted-aminomethyl)phenyl]-1,10-phenanthroline derivatives was synthesized, and the compounds were screened in vitro against three protozoan parasites (Plasmodium falciparum, Leishmania donovani, Trypanosoma brucei brucei). Biological results showed antiparasitic activity with IC50 values μm range. The cytotoxicity these molecules assessed by incubation human HepG2 cells; for some derivatives, observed at significantly higher concentrations than activity. 1h...
A series of new 2,4-bis[(substituted-aminomethyl)phenyl]quinoline, 1,3-bis[(substituted-aminomethyl)phenyl]isoquinoline, and 2,4-bis[(substituted-aminomethyl)phenyl]quinazoline derivatives was designed, synthesised, evaluated in vitro against three protozoan parasites (Plasmodium falciparum, Leishmania donovani, Trypanosoma brucei brucei). Biological results showed antiprotozoal activity with IC50 values the µM range. In addition, cytotoxicity these original molecules assessed human HepG2...
Human malaria infection begins with a one-time asymptomatic liver stage followed by cyclic symptomatic blood stage. For decades, the research for novel antimalarials focused on high-throughput screening of molecules that only targeted asexual stages. In search new effective compounds presenting triple action against erythrocytic and stages in addition to ability block transmission disease via mosquito vector, 2-amino-thienopyrimidinone derivatives were synthesized tested their antimalarial...
The synthesis in water of new sulfone derivatives under microwave irradiation is described. This eco-friendly process leads to the expected products good yields by reaction various substituted sulfinates (commercially available or obtained reduction corresponding sulfonyl chlorides) with 4-chloromethyl-2-methyl-5-nitro-1,3-thiazole. In order evaluate antiproliferative effect these compounds, several are also dichlorinated on Cα next group. An evaluation different cancer cell lines reveals...
By taking into account our previously described series of 1,3,5-tris[(4-(substituted-aminomethyl)phenyl)methyl]benzene compounds, we have now designed, prepared, and evaluated in vitro against Plasmodium falciparum a novel structural analogues these molecules, i.e., the 1,3,5-tris[(4-(substituted-aminomethyl)phenoxy)methyl]benzene derivatives. The pharmacological data showed antimalarial activity with IC50 values sub μM range. cytotoxicity new nitrogen polyphenoxymethylbenzene compounds was...
We report herein a simple and efficient two-step synthetic approach to new 2-trichloromethylquinazolines possessing variously substituted sulfonamide group at position 4 used prepare quinazolines with antiparasitic properties. Thus, an original series of 20 derivatives was synthesized, which proved be less-toxic than previously synthesized hits on the human HepG2 cell line, but did not display significant antiplasmodial activity. A brief Structure-Activity Relationship (SAR) evaluation shows...
A series of novel 2,9-bis[(substituted-aminomethyl)]-4,7-phenyl-1,10-phenanthroline derivatives was designed, synthesized, and evaluated in vitro against three protozoan parasites (Plasmodium falciparum, Leishmania donovani Trypanosoma brucei brucei). Pharmacological results showed antiprotozoal activity with IC50 values the sub μM range. In addition, cytotoxicity these original molecules assessed human HepG2 cells. The substituted diphenylphenanthroline 1l identified as most potent...
Following our search for antimalarial compounds, novel series of piperazinylalcohol pyrrolo[ 1,2-a]quinoxaline derivatives 1-2 were synthesized from 2-nitroaniline or 2-amino-3- nitrophenol and tested in vitro activity upon the intraerythrocytic stage W2 3D7 Plasmodium falciparum strains. Biological results showed good with IC50 ranging 0.3 to 21.1 µM. In attempting investigate large broad-spectrum antiprotozoal activities these pyrrolo[1,2-a]quinoxaline derivatives, their properties toward...
A series of new 2,9-bis[(pyridinylalkylaminomethyl)phenyl]-1,10-phenanthroline compounds was considered, synthesized, and evaluated in vitro against three parasites (Plasmodium falciparum, Leishmania donovani Trypanosoma brucei brucei).Pharmacological results showed antiparasitic activity with IC 50 values the sub µM range.The cytotoxicity these novel aza derivatives on human HepG2 cells.The phenanthroline 1f noticed as most potent antimalarial candidate a ratio cytotoxic to antiprotozoal...