N'est plus au Laboratoire.
BENFODDA Zohra
Fonction : Doctorant
Thème de Recherche: Synthèses Stéréosélectives & Acides Aminés Modifiés
zohra.benfodda
unimes.fr
0467143843
Bureau: 0, Bât: 17 - Site : UM2
Domaines de Recherche: - Chimie/Chimie organique
- Chimie/Chimie thérapeutique
- Sciences du Vivant/Cancer
- Chimie/Chemo-informatique
- Sciences du Vivant/Biochimie, Biologie Moléculaire/Biochimie
- Sciences du Vivant/Biochimie, Biologie Moléculaire/Biologie moléculaire
- Sciences du Vivant/Médecine humaine et pathologie/Endocrinologie et métabolisme
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Dernieres productions scientifiques :
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Synthesis, Anticancer Activity and Computational SAR Analysis of Acylsulfonylpiperazines Derivatives
Auteur(s): Benfodda Z., Fritz Vanessa, Henriquet Corinne, Fattorusso Caterina, Cebrian-Torrejon Gerardo, Persico Marco, Dato Antonio, Menna Marialuisa, Blancou H., Fajas Lluis
(Article) Publié:
Medicinal Chemistry, vol. 7 p.257-267 (2017)
Ref HAL: hal-01662364_v1
DOI: 10.4172/2161-0444.1000466
Résumé: A series of 1-acyl-4-sulfonylpiperazine derivatives has been prepared. The antiproliferative effect of these compounds was evaluated in vitro against human prostate cancer cell line C4-2, several among them exhibited interesting growth inhibitory against this particular cell line. Finally, a molecular modeling study was employed to analyze the structure/activity relationships (SAR) of these novel compounds..
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The Rational Design, Synthesis, and Antimicrobial Properties of Thiophene Derivatives That Inhibit Bacterial Histidine Kinases
Auteur(s): Boibessot T., zschiedrich Christopher, Lebeau A., Bénimélis David, Dunyach-Remy Catherine, Lavigne Jean-Philippe, Szurmant Hendrik, Benfodda Z., Meffre P.
(Article) Publié:
European Journal Of Medicinal Chemistry, vol. p.8830-8847 (2016)
Ref HAL: hal-01543599_v1
DOI: 10.1021/acs.jmedchem.6b00580
Résumé: The emergence of multidrug-resistant bacteria emphasizes the urgent need for novel antibacterial compounds targeting unique cellular processes. Two-component signal transduction systems (TCSs) are commonly used by bacteria to couple environmental stimuli to adaptive responses, are absent in mammals, and are embedded in various pathogenic pathways. To attenuate these signaling pathways, we aimed to target the TCS signal transducer histidine kinase (HK) by focusing on their highly conserved adenosine triphosphate-binding domain. We used a structure-based drug design strategy that begins from an inhibitor-bound crystal structure and includes a significant number of structurally simplifiying “intuitive” modifications to arrive at the simple achiral, biaryl target structures. Thus, ligands were designed, leading to a series of thiophene derivatives. These compounds were synthesized and evaluated in vitro against bacterial HKs. We identified eight compounds with significant inhibitory activities against these proteins, two of which exhibited broad-spectrum antimicrobial activity. The compounds were also evaluated as adjuvants for the treatment of resistant bacteria. One compound was found to restore the sensivity of these bacteria to the respective antibiotics.
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Part I: preparations of ethynylglycine synthon
Auteur(s): Benfodda Z., Bénimélis David, Reginato Gianna, Meffre P.
(Article) Publié:
Amino Acids, vol. 47 p.271-279 (2015)
Ref HAL: hal-01676812_v1
DOI: 10.1007/s00726-014-1902-0
Résumé: The ethynylglycine synthon {(R)-2,2-dimethyl-3-(tert-butoxycarbonyl)-4-ethynyloxazolidine} is a chiral compound with valuable synthetic interest. An update on the different routes for its synthesis is reviewed and discussed.
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Metabolic intervention on lipid synthesis converging pathways abrogates prostate cancer growth
Auteur(s): Fritz Vivian, Benfodda Z., Henriquet C., Hure S, Cristol Jean Paul, Michel Françoise, Carbonneau M-A, Casas F, Fajas L.
(Article) Publié:
Oncogene, vol. 32 p.5101-5110 (2013)
Ref HAL: hal-01274921_v1
DOI: 10.1038/onc.2012.523
Résumé: One of the most conserved features of all cancers is a profound reprogramming of cellular metabolism, favoring biosynthetic processes and limiting catalytic processes. With the acquired knowledge of some of these important changes, we have designed a combination therapy in order to force cancer cells to use a particular metabolic pathway that ultimately results in the accumulation of toxic products. This innovative approach consists of blocking lipid synthesis, at the same time that we force the cell, through the inhibition of AMP-activated kinase, to accumulate toxic intermediates, such as malonyl-coenzyme A (malonyl-CoA) or nicotinamide adenine dinucleotide phosphate. This results in excess of oxidative stress and cancer cell death. Our new therapeutic strategy, based on the manipulation of metabolic pathways, will certainly set up the basis for new upcoming studies defining a new paradigm of cancer treatment.
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New developments in the synthesis of acetylenic analogues of glutamate
Auteur(s): Meffre P., Benfodda Z., Bénimélis David, Rolland-Fulcrand V., Acher Francine
Conference: 12 th International Congress on Amino Acids, Peptides and Proteins (Beijing, CN, 2011-08-01)
Actes de conférence: Amino Acids, vol. 41 p.S79 (2011)
Ref HAL: hal-00621161_v1
Résumé: Glutamate ((S)-Glu)is the major excitatory amino acid in the central nervous system. It acts by stimulating ionotropic and metabotropic glutamate receptors (iGluR and mGluR respectively). Glutamate has been shown to be involved not only in many neuropathologies such as anxiety, pain, ischemia, Parkinson's disease, epilepsy and schizophrenia. More recently, mGlu receptors have also been detected in non-neuronal cells suggesting that they could be implicated in carcinogenesis. mGlu receptors are G-protein-coupled receptors and eight subtypes (mGluR1 to 8) have been identified and classified into three groups (I-III) based upon sequence homology, transduction mechanism and pharmacological profile. Because of their modulating properties, mGlu receptors are recognized as promising therapeutic targets and many ligands (agonists and antagonists) have been prepared to better understand the pharmacology of mGlu receptors in order to selectively activate the different groups and subtypes of receptors. An -amino acid moiety can be found in all mGlu receptors competitive ligands and most of the side chains hold an acidic function. Examination of the glutamate binding site in the mGlu receptors and pharmacological data of some ligands shows that sterically constrained structures with an optimal distance between functional groups could lead to potent and selective new ligands. It is known that introducing an unsaturation in a biologically active structure could modify the conformation of the molecule and thus the biological activity. In this respect, the synthesis of new acetylenic analogues of glutamate will be described.
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