Christian Bailly
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View article: A new horizon for the anesthetic drug dyclonine
A new horizon for the anesthetic drug dyclonine Open
For more than sixty years, the piperidinopropiophenone derivative dyclonine is used as a local anesthetic in human and veterinary medicines. Dyclonine-containing drugs (Dyclone, DycloPro) have been developed as anti-itching medications and…
View article: Anticancer Activity of Demethylincisterol A3 and Related Incisterol-Type Fungal Products
Anticancer Activity of Demethylincisterol A3 and Related Incisterol-Type Fungal Products Open
Highly degraded sterols belonging to the incisterol group have been identified in a large set of microorganisms. The leading product in the family is demethylincisterol A3 (DM-A3), isolated from various fungi and endowed with marked antitu…
View article: Pharmacognosy and natural product chemistry of the marine sponge Hyrtios erectus
Pharmacognosy and natural product chemistry of the marine sponge Hyrtios erectus Open
Marine-derived bioactive natural products are an essential resource for drug discovery. In particular, marine sponges and associated symbionts can be exploited to discover innovative compounds and new drug candidates. The sponge Hyrtios er…
View article: Insights into the Bioactivities and Mechanism of Action of the Microbial Diketopiperazine Cyclic Dipeptide Cyclo(L-leucyl-L-prolyl)
Insights into the Bioactivities and Mechanism of Action of the Microbial Diketopiperazine Cyclic Dipeptide Cyclo(L-leucyl-L-prolyl) Open
Diketopiperazines (DKPs) are biologically important cyclic dipeptides widespread in nature, associated primarily with microorganisms. This is the case for the 2,5-DKP derivative cyclo(L-Leu-L-Pro) (cLP), also known as gancidin W or PPDHMP,…
View article: Withangulatin A Identified as a Covalent Binder to Zap70 Kinase by Molecular Docking
Withangulatin A Identified as a Covalent Binder to Zap70 Kinase by Molecular Docking Open
Inhibitors of the tyrosine kinase Zap70 are actively searched to improve treatments of lymphoid malignancies and autoimmune diseases associated with an abnormal T-cell response. The natural product withaferin A (WFA) has been characterized…
View article: The utility of next generation sequencing targeted multigene panels in the Adult Neurogenetic Clinic at Tygerberg Hospital, South Africa
The utility of next generation sequencing targeted multigene panels in the Adult Neurogenetic Clinic at Tygerberg Hospital, South Africa Open
View article: Biological and Medicinal Properties of Chrysanthemum boreale Makino and Its Bioactive Products
Biological and Medicinal Properties of Chrysanthemum boreale Makino and Its Bioactive Products Open
Chrysanthemum species represent an economically important group of flowering plants. Many species also present a medicinal interest, notably for the treatment of inflammatory pathologies. This is the case for Chrysanthemum boreale Makino, …
View article: On the Molecular Origin of the Toxicity of Erophaca baetica (L.) Boiss.
On the Molecular Origin of the Toxicity of Erophaca baetica (L.) Boiss. Open
Background/Objectives: The plant species Erophaca baetica (L.) Boiss. (synonym: Astragalus lusitanicus Lam.) is found essentially around the Mediterranean basin, with Morocco as its ancestral territory. The foliage of E. baetica is toxic t…
View article: Interaction of brequinar and analogs with PD-L1: a molecular docking analysis
Interaction of brequinar and analogs with PD-L1: a molecular docking analysis Open
Aim: The immunosuppressive drug brequinar (BQR) is a potent inhibitor of dihydroorotate dehydrogenase (DHODH) active against autoimmune diseases and viral infections. This oral drug is currently evaluated for the treatment of cancers, nota…
View article: Isolation, synthesis, mechanism of action, and pharmacological activities of bisabolangelone and related bisabolenoids
Isolation, synthesis, mechanism of action, and pharmacological activities of bisabolangelone and related bisabolenoids Open
View article: HR‐MS Analysis of the Covalent Binding of Edaravone to 5‐Formylpyrimidine Bases and a DNA Oligonucleotide Containing a 5‐Formylcytidine Residue
HR‐MS Analysis of the Covalent Binding of Edaravone to 5‐Formylpyrimidine Bases and a DNA Oligonucleotide Containing a 5‐Formylcytidine Residue Open
Rationale Edaravone (EDA) is a radical scavenger and an antioxidant drug approved to treat amyotrophic lateral sclerosis and used as a research tool to explore treatment of neurodegenerative diseases and cancers. It is also a reactive agen…
View article: Benzoxanthenone Lignans Related to Carpanone, Polemanone, and Sauchinone: Natural Origin, Chemical Syntheses, and Pharmacological Properties
Benzoxanthenone Lignans Related to Carpanone, Polemanone, and Sauchinone: Natural Origin, Chemical Syntheses, and Pharmacological Properties Open
Medicinal plants from the genus Saururus are commonly used to treat inflammatory pathologies. They contain numerous bioactive compounds, notably the polycyclic lignan sauchinone from the species Saururus chinensis. An in-depth analysis of …
View article: Interaction of Asparagusic Acid, Asparaptines and Related Dithiolane Derivatives With Angiotensin‐Converting Enzyme‐2 (ACE‐2): A Molecular Docking Study
Interaction of Asparagusic Acid, Asparaptines and Related Dithiolane Derivatives With Angiotensin‐Converting Enzyme‐2 (ACE‐2): A Molecular Docking Study Open
A variety of sulfur‐containing small molecules can be found in the spears of asparagus ( Asparagus Officinalis L.) including compounds derived from asparagusic acid such as the amino acid derivatives asparaptines A, B, and C. The previous …
View article: Interaction of Microcolin Cyanobacterial Lipopeptides with Phosphatidylinositol Transfer Protein (PITP)—Molecular Docking Analysis
Interaction of Microcolin Cyanobacterial Lipopeptides with Phosphatidylinositol Transfer Protein (PITP)—Molecular Docking Analysis Open
Background/Objectives: Microcolins A–M are cytotoxic marine lipopeptides produced by the cyanobacterium Moorena producens, also known as Lyngbya majuscula. Recent studies have shown that two compounds in the series, microcolins B and H, ca…
View article: Overview of the Ruspolia Plant Genus: Insights into Its Chemical Diversity and Biological Potential
Overview of the Ruspolia Plant Genus: Insights into Its Chemical Diversity and Biological Potential Open
The genus Ruspolia refers to a small group of plants in the Acanthaceae family, with two dominant species R. decurrens and R. hypocrateriformis essentially distributed in tropical parts of Africa. Decoctions from these plants are used in f…
View article: Design, synthesis and evaluation of pyrimidinobenzylamide and pyrimidinothiophenamide derivatives as inhibitors of DOT1L and related epigenetic targets DNMT3a, PRMT4 and other HMTs
Design, synthesis and evaluation of pyrimidinobenzylamide and pyrimidinothiophenamide derivatives as inhibitors of DOT1L and related epigenetic targets DNMT3a, PRMT4 and other HMTs Open
In silico based design and synthesis of non-nucleosidic DOT1L inhibitors is presented. SAR led to the identification of key moieties. The compounds were evaluated on related epigenetic targets and μM-range potency hit inhibitors were ident…
View article: Alkaloids from Mackinlaya species and synthetic mackinazolinone derivatives: An overview
Alkaloids from Mackinlaya species and synthetic mackinazolinone derivatives: An overview Open
Mackinazolinone is the main alkaloid isolated from plants of the genus Mackinlaya, essentially distributed in tropical Asia and Australia. There are five Mackinlaya species all containing bioactive alkaloids with a tetrahydropyridoquinazol…
View article: A systematic review of proaporphine alkaloids and a pharmacological update
A systematic review of proaporphine alkaloids and a pharmacological update Open
Background: Proaporphine alkaloids are present in many plant families. They are often considered as metabolic precursors to aporphines. They generally contain a cyclohexadienone system and can rearrange to aporphines on treatment with acid…
View article: A Capacity Audit of Medical Geneticists and Genetic Counsellors in South Africa, 2024: A National Crisis
A Capacity Audit of Medical Geneticists and Genetic Counsellors in South Africa, 2024: A National Crisis Open
Community genetic services were introduced in South Africa almost seven decades ago, with medical geneticists and genetic counsellors being formally recognized for the past 30 years. Initial training platforms were established at academic …
View article: Covalent binding of withanolides to cysteines of protein targets
Covalent binding of withanolides to cysteines of protein targets Open
Withanolides represent an important category of natural products with a steroidal lactone core. Many of them contain an α,β-unsaturated carbonyl moiety with a high reactivity toward sulfhydryl groups, including protein cysteine thiols. Dif…
View article: Synthesis, Molecular Electron Density Theory Study, Molecular Docking, and Pharmacological Evaluation of New Coumarin–Sulfonamide–Nitroindazolyl–Triazole Hybrids as Monoamine Oxidase Inhibitors
Synthesis, Molecular Electron Density Theory Study, Molecular Docking, and Pharmacological Evaluation of New Coumarin–Sulfonamide–Nitroindazolyl–Triazole Hybrids as Monoamine Oxidase Inhibitors Open
Inhibitors of monoamine oxidases (MAOs) are of interest for the treatment of neurodegenerative disorders and other human pathologies. In this frame, the present work describes different synthetic strategies to obtain MAO inhibitors via the…
View article: Interaction of norsecurinine-type monomeric and dimeric alkaloids with α-tubulin: a molecular docking study
Interaction of norsecurinine-type monomeric and dimeric alkaloids with α-tubulin: a molecular docking study Open
Aim: New microtubule-targeting agents are needed to improve cancer treatment. The recent characterization of the anticancer alkaloid securinine as a tubulin-binding agent prompted us to explore the interaction of related monomeric and dime…
View article: Activity of pyridyl-pyrazolone derivatives against Trypanosoma cruzi
Activity of pyridyl-pyrazolone derivatives against Trypanosoma cruzi Open
New affordable drugs are needed for the treatment of infection with the protozoan parasite Trypanosoma cruzi responsible for the Chagas disease (CD). Only two old drugs are currently available, nifurtimox and benznidazole (Bz) but they exh…
View article: Withania frutescens (L.) Pauquy, a valuable Mediterranean shrub containing bioactive withanolides
Withania frutescens (L.) Pauquy, a valuable Mediterranean shrub containing bioactive withanolides Open
The bushy plant Withania frutescens (L.) Pauquy is well distributed in the West-Mediterranean area, notably in the south of Spain, Algeria and Morocco where is it is used traditionally for the treatment of various human diseases, including…
View article: Interaction of Norsecurinine-Type Oligomeric Alkaloids with α-Tubulin: A Molecular Docking Study
Interaction of Norsecurinine-Type Oligomeric Alkaloids with α-Tubulin: A Molecular Docking Study Open
The medicinal plant Securinega virosa (Roxb ex. Willd) Baill., also known as Flueggea virosa (Roxb. ex Willd.) Royle, is commonly used in traditional medicine in Africa and Asia for the management of diverse pathologies, such as parasite i…
View article: Limonoids isolated from <i>Chisocheton ceramicus</i> <scp>Miq.</scp> and the antiadipogenic mechanism of action of ceramicine B
Limonoids isolated from <i>Chisocheton ceramicus</i> <span>Miq.</span> and the antiadipogenic mechanism of action of ceramicine B Open
Different types of limonoids have been isolated from plants of the Chisocheton genus, notably from the species Chisocheton ceramicus Miq. which is largely distributed in the Indonesian archipelago and Malaysia region. A variety of natural …
View article: A molecular docking exploration of the large extracellular loop of tetraspanin CD81 with small molecules
A molecular docking exploration of the large extracellular loop of tetraspanin CD81 with small molecules Open
View article: Insights into the Mechanism of Action of the Degraded Limonoid Prieurianin
Insights into the Mechanism of Action of the Degraded Limonoid Prieurianin Open
Limonoids are extremely diversified in plants, with many categories of products bearing an intact, rearranged or fragmented oxygenated scaffold. A specific subgroup of fragmented or degraded limonoids derives from the tetranortriterpenoid …
View article: Application of the Rumsfeld matrix to anticancer natural product target discovery
Application of the Rumsfeld matrix to anticancer natural product target discovery Open