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View article: Acetylcholinesterase as a Target for Heliotridine-Type Alkaloids Isolated from Plants: A Computational Study
Acetylcholinesterase as a Target for Heliotridine-Type Alkaloids Isolated from Plants: A Computational Study Open
The enzyme acetylcholinesterase (AChE) acts in mammalians and insects. Its inhibitors are considered to treat human disease and to develop insecticides. Docking calculations were performed by using AutoDock Vina and Protein–Ligand ANTSyste…
View article: 3a-(4-Chlorophenyl)-1-thioxo-2,3,3a,4-tetrahydroimidazo[1,5-a]quinazolin-5(1H)-one
3a-(4-Chlorophenyl)-1-thioxo-2,3,3a,4-tetrahydroimidazo[1,5-a]quinazolin-5(1H)-one Open
With the aim of producing new heterocycle molecules, the previously reported 2-(aminomethyl)-2-(4-chlorophenyl)-2,3-dihydroquinazolin-4(1H)-one was converted efficiently by reacting with N,N′-dithiocarbonyldiimidazole (DTCI) to produce the…
View article: 3a-(4-Chlorophenyl)-1-thioxo-2,3,3a,4-tetrahydroimidazo[1,5-a]quinazolin-5(1H)-one
3a-(4-Chlorophenyl)-1-thioxo-2,3,3a,4-tetrahydroimidazo[1,5-a]quinazolin-5(1H)-one Open
With the aim to produce new heterocycle molecules, the previously reported 2-(aminomethyl)-2-(4-chlorophenyl)-2,3-dihydroquinazolin-4(1H)-one was converted efficiently by reacting with N,N’-dithiocarbonyldiimidazole (DTCI), to produce the …
View article: EGCG Disrupts the LIN28B/Let-7 Interaction and Reduces Neuroblastoma Aggressiveness
EGCG Disrupts the LIN28B/Let-7 Interaction and Reduces Neuroblastoma Aggressiveness Open
Neuroblastoma (NB) is the most commonly diagnosed extracranial solid tumor in children, accounting for 15% of all childhood cancer deaths. Although the 5-year survival rate of patients with a high-risk disease has increased in recent decad…
View article: Structural Insights into the Marine Alkaloid Discorhabdin G as a Scaffold towards New Acetylcholinesterase Inhibitors
Structural Insights into the Marine Alkaloid Discorhabdin G as a Scaffold towards New Acetylcholinesterase Inhibitors Open
In this study, Antarctic Latrunculia sponge-derived discorhabdin G was considered a hit for developing potential lead compounds acting as cholinesterase inhibitors. The hypothesis on the pharmacophore moiety suggested through molecular doc…
View article: A Comprehensive Computational NMR Analysis of Organic Polyarsenicals including the Marine Sponge-Derived Arsenicins A–D and Their Synthetic Analogs
A Comprehensive Computational NMR Analysis of Organic Polyarsenicals including the Marine Sponge-Derived Arsenicins A–D and Their Synthetic Analogs Open
The adamantane structure of arsenicin A and nor-adamantane structures of arsenicins B–D have gained attention as unique natural polyarsenicals, as well as hits showing promising anticancer activity. The purpose of this study is to apply th…
View article: 3a-(4-Chlorophenyl)-1-methyl-3a,4-dihydroimidazo[1,5-a]quinazolin-5(3H)-one: Synthesis and In Silico Evaluation as a Ligand in the µ-Opioid Receptor
3a-(4-Chlorophenyl)-1-methyl-3a,4-dihydroimidazo[1,5-a]quinazolin-5(3H)-one: Synthesis and In Silico Evaluation as a Ligand in the µ-Opioid Receptor Open
In the search for fused heterocycle molecules with potential biological activities, the new title compound was produced in racemic form via a four step-synthetic sequence with an overall yield of 60%. It was structurally characterised via …
View article: Expanding the Chemical Space of Arsenicin A-C Related Polyarsenicals and Evaluation of Some Analogs as Inhibitors of Glioblastoma Stem Cell Growth
Expanding the Chemical Space of Arsenicin A-C Related Polyarsenicals and Evaluation of Some Analogs as Inhibitors of Glioblastoma Stem Cell Growth Open
The marine polyarsenical metabolite arsenicin A is the landmark of a series of natural and synthetic molecules characterized by an adamantane-like tetraarsenic cage. Arsenicin A and related polyarsenicals have been evaluated for their anti…
View article: Hybrid Molecules Containing Naphthoquinone and Quinolinedione Scaffolds as Antineoplastic Agents
Hybrid Molecules Containing Naphthoquinone and Quinolinedione Scaffolds as Antineoplastic Agents Open
In recent decades, molecular hybridization has proven to be an efficient tool for obtaining new synthetic molecules to treat different diseases. Based on the core idea of covalently combining at least two pharmacophore fragments present in…
View article: The Promising Role of Natural Products in Drug Discovery
The Promising Role of Natural Products in Drug Discovery Open
View article: LC-ESI/MS-Phytochemical Profiling with Antioxidant, Antibacterial, Antifungal, Antiviral and In Silico Pharmacological Properties of Algerian Asphodelus tenuifolius (Cav.) Organic Extracts
LC-ESI/MS-Phytochemical Profiling with Antioxidant, Antibacterial, Antifungal, Antiviral and In Silico Pharmacological Properties of Algerian Asphodelus tenuifolius (Cav.) Organic Extracts Open
Asphodelus tenuifolius Cav. (A. tenuifolius) is a medicinal plant with a long history of traditional use to treat ailments. In this study, total phenolic and flavonoid content evaluation using LC-ESI/MS analysis and various biological acti…
View article: DNA-Binding Properties of Cytotoxic Naphtindolizinedione-Carboxamides Acting as Type II Topoisomerase Inhibitors. A Combined In Silico and Experimental Study
DNA-Binding Properties of Cytotoxic Naphtindolizinedione-Carboxamides Acting as Type II Topoisomerase Inhibitors. A Combined In Silico and Experimental Study Open
Some clinically-used anticancer drugs are DNA intercalators acting as topoisomerase (Topo) IIα poisons in tumor cells highly expressing the enzyme. Synthetic naphtindolizinedione-carboxamides, previously designed as potential antitumor age…
View article: CCDC 2006352: Experimental Crystal Structure Determination
CCDC 2006352: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2006351: Experimental Crystal Structure Determination
CCDC 2006351: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Structural Isomerism and Enhanced Lipophilicity of Pyrithione Ligands of Organoruthenium(II) Complexes Increase Inhibition on AChE and BuChE
Structural Isomerism and Enhanced Lipophilicity of Pyrithione Ligands of Organoruthenium(II) Complexes Increase Inhibition on AChE and BuChE Open
The increasing number of Alzheimer’s disease (AD) cases requires the development of new improved drug candidates, possessing the ability of more efficient treatment as well as less unwanted side effects. Cholinesterase enzymes are highly a…
View article: Design, Synthesis and Antimicrobial Evaluation of New Norfloxacin-Naphthoquinone Hybrid Molecules
Design, Synthesis and Antimicrobial Evaluation of New Norfloxacin-Naphthoquinone Hybrid Molecules Open
Although the wide arsenal of drugs available to treat bacterial infections, emerging drugresistant bacterial pathogens have recently highlighted an urgent need to find new more effective and less toxic therapeutic agents. Fluoroquinolones,…
View article: Actinobacteria Derived from Algerian Ecosystems as a Prominent Source of Antimicrobial Molecules
Actinobacteria Derived from Algerian Ecosystems as a Prominent Source of Antimicrobial Molecules Open
Actinobacteria, in particular “rare actinobacteria” isolated from extreme ecosystems, remain the most inexhaustible source of novel antimicrobials, offering a chance to discover new bioactive metabolites. This is the first overview on acti…
View article: Design, Synthesis and Cancer Cell Growth Inhibition Evaluation of New Aminoquinone Hybrid Molecules
Design, Synthesis and Cancer Cell Growth Inhibition Evaluation of New Aminoquinone Hybrid Molecules Open
Molecular hybridization has proven to be a successful multi-target strategy in the design and development of new antitumor agents. Based on this rational approach, we have planned hybrid molecules containing covalently linked pharmacophori…
View article: Modeling improved production of the chemotherapeutic polypeptide actinomycin D by a novel Streptomyces sp. strain from a Saharan soil
Modeling improved production of the chemotherapeutic polypeptide actinomycin D by a novel Streptomyces sp. strain from a Saharan soil Open
The novel bioactive actinobacterial strain GSBNT10 obtained from a Saharan soil, was taxonomically characterized using a polyphasic approach. 16S rRNA gene sequence analysis supported the classification of the isolate within the genus S…
View article: Enhanced Production and Quantitative Evaluation of Nigericin from the Algerian Soil-Living Streptomyces youssoufiensis SF10 Strain
Enhanced Production and Quantitative Evaluation of Nigericin from the Algerian Soil-Living Streptomyces youssoufiensis SF10 Strain Open
Nigericin, one of the main ionophoric polyethers produced by various Streptomyces strains, presents relevant biological activities including antibacterial and recently studied antitumor properties. This work describes the influence of diff…
View article: Synthesis of 2,6-Diamino-Substituted Purine Derivatives and Evaluation of Cell Cycle Arrest in Breast and Colorectal Cancer Cells
Synthesis of 2,6-Diamino-Substituted Purine Derivatives and Evaluation of Cell Cycle Arrest in Breast and Colorectal Cancer Cells Open
Reversine is a potent antitumor 2,6-diamino-substituted purine acting as an Aurora kinases inhibitor and interfering with cancer cell cycle progression. In this study we describe three reversine-related molecules, designed by docking calcu…
View article: Nigericin and grisorixin methyl ester from the Algerian soil-living <i>Streptomyces youssoufiensis</i> SF10 strain: a computational study on their epimeric structures and evaluation of glioblastoma stem cells growth inhibition
Nigericin and grisorixin methyl ester from the Algerian soil-living <i>Streptomyces youssoufiensis</i> SF10 strain: a computational study on their epimeric structures and evaluation of glioblastoma stem cells growth inhibition Open
The present work describes the metabolites produced by a strain identified as Streptomyces youssoufiensis, whose secondary metabolites profile has not been studied so far. The crude ethyl acetate extract was analyzed by high performance li…
View article: Synthesis and in-vitro anticancer evaluation of polyarsenicals related to the marine sponge derived Arsenicin A
Synthesis and in-vitro anticancer evaluation of polyarsenicals related to the marine sponge derived Arsenicin A Open
In the light of the promising bioactivity of the tetraarsenic marine metabolite arsenicin A, the dimethyl analogue 2 and four isomeric methylene homologues (including the natural product itself) were obtained using a one-pot microwave-assi…
View article: Microwave-assisted synthesis of new imide- and formamide-derivatives of 2(3H)-benzoxazolinones and 2(3H)-benzothiazolinones
Microwave-assisted synthesis of new imide- and formamide-derivatives of 2(3H)-benzoxazolinones and 2(3H)-benzothiazolinones Open
With the aim to obtain 2(3H)-benzoxazolinones and 2(3H)-benzothiazolinone derivatives, we synthesized new imide compounds 5a-c, 6c-d and 7a-d by treating their 6-amino precursors with succinic, maleic or phthalic anhydride.The microwave (M…
View article: Discorhabdin alkaloids from Antarctic Latrunculia spp. sponges as a new class of cholinesterase inhibitors
Discorhabdin alkaloids from Antarctic Latrunculia spp. sponges as a new class of cholinesterase inhibitors Open
View article: <strong>Efficient TBD-Catalyzed Synthesis of Capsaicin-like Molecules </strong>
<strong>Efficient TBD-Catalyzed Synthesis of Capsaicin-like Molecules </strong> Open
Capsaicin, the natural compound responsible for the spicy flavor in pepper fruits, has shown antioxidant and weight-reductive properties, cardiovascular benefits, anti-carcinogenic activity and recently pain relief effects. Studies on a se…
View article: Antibacterial polyketide from the marine alga-derived endophitic Streptomyces sundarbansensis: a study on hydroxypyrone tautomerism
Antibacterial polyketide from the marine alga-derived endophitic Streptomyces sundarbansensis: a study on hydroxypyrone tautomerism Open
Polyketide 13 [=2-hydroxy-5-((6-hydroxy-4-oxo-4H-pyran-2-yl)methyl)-2-propylchroman-4-one] and three related
\nknown compounds 7, 9 and 11 were obtained and structurally characterized from Streptomyces sundarbansensis strain,
\nan endophyt…
View article: Muscarine-like compounds derived from a pyrolysis product of cellulose
Muscarine-like compounds derived from a pyrolysis product of cellulose Open
Starting from a hydroxylactone anhydrosugar available from catalytic cellulose pyrolysis, five new muscarine-like compounds have been synthesized and studied for their binding affinity to human subtype muscarine receptors, obtaining result…