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Synthesis and Biological Evaluation of Fused [1,2,3]Triazolo[4ʹ,5ʹ:4,5]pyrido[2,3-d]pyrimidine Linked 1,2,3-Triazolesas Potent EGFR Targeting Anticancer Agents
AbstractUsing 1-(4-nitrophenyl)-4,5-dihydro-1 H -[1,2,3]triazolo[4ʹ,5ʹ:4,5]pyrido[2,3- d ]pyrimidine and various aryl azides, we developed and...
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Synthesis of Novel 2-((3-(Benzofuran-2-yl)-1-phenyl-1H-pyrazol-4-yl)methylene)hydrazinyl-4-phenylthiazole: Potent EGFR Targeting Anticancer Agents
AbstractObjective: Benzofurans, fused pyrazole systems, and thiazole moieties are the most important pharmacophores and intermediates for making...
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Ugi 5-center-4-component reaction of α-amino aldehydes and its application in synthesis of 2-oxopiperazines
A synthetic route leading to densely functionalized 2-oxopiperazines is presented. The strategy employs a 5-center-4-component variant of Ugi...
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Synthesis, Characterization of Formazan Derivatives from Isoniazid and Study Their Antioxidant Activity and Molecular Docking
AbstractObjective: Synthesis, Characterization of formazan derivatives and studies the antioxidant activity of prepared compounds and molecular...
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An efficient synthesis of phosphonated cyclopentenones by NaN3-catalyzed three-component reaction between trialkyl phosphites, ethyl arylmethylidenecyanoacetates and dialkyl acetylenedicarboxylates
NaN 3 -catalysed three-component reaction between trialkyl phosphites, dialkyl acetylenedicarboxylates and ethyl arylmethylidenecyanoacetates afforded...
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Synthesis of Chromeno[2,3-d]pyrimidine-2,4(3H)-dion Derivatives Fused with Indole Moiety as Potent Biological Agents
AbstractObjective: In this paper we have reported the synthesis of novel chromeno[2,3- d ]pyrimidine-2,4(3 H )dione derivatives ( IVa–IVh ) by three...
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Structure-based drug design and characterization of novel pyrazine hydrazinylidene derivatives with a benzenesulfonate scaffold as noncovalent inhibitors of DprE1 tor tuberculosis treatment
In this study, we present a novel series of ( E )-4-((2-(pyrazine-2-carbonyl) hydrazineylidene)methyl)phenyl benzenesulfonate (T1-T8) and 4-(( E )-((( Z )-a...
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Griseofulvin enantiomers and bromine-containing griseofulvin derivatives with antifungal activity produced by the mangrove endophytic fungus Nigrospora sp. QQYB1
Marine microorganisms have long been recognized as potential sources for drug discovery. Griseofulvin was one of the first antifungal natural...
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Design, synthesis, and biological evaluation of new biaryl derivatives of cycloalkyl diacetamide bearing chalcone moiety as type II c-MET kinase inhibitors
Many human cancers have been associated with the deregulation of the mesenchymal-epithelial transition factor tyrosine kinase (MET) receptor, a...
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Design, Synthesis and Biological Evaluation of Novel 1H-1,2,4-Triazole Derivatives as Strigolactone Biosynthesis Inhibitors
Strigolactone (SL) biosynthesis inhibitors have shown impressive activity in increasing shoot branching and inhibiting seed germination of the root...
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One-pot synthesis, characterization and antiviral properties of new benzenesulfonamide-based spirothiazolidinones
A novel series of benzenesulfonamide substituted spirothiazolidinone derivatives ( 3a–j ) were synthesized, characterized and evaluated for their...
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Hfq C-terminal region forms a β-rich amyloid-like motif without perturbing the N-terminal Sm-like structure
Hfq is a pleitropic actor that serves as stress response and virulence factor in the bacterial cell. To execute its multiple functions, Hfq assembles...
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Synthesis, Characterization of Novel Thiazole Hydrazine Derivatives, and Inhibitory Action Against the VEGFR-2
AbstractObjective: Synthesis, characterization of novel thiazole hydrazine derivatives and inhibitory action against the VEGFR-2. Methods: The novel...
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Synthesis, Identification, Antioxidant, Molecular Docking, and In Silico ADME Study for Some New Derivatives Containing Thiourea Moiety
AbstractObjective: Synthesized a series of new thiourea (TU) derivatives, tested their antioxidant activity, and investigated their expected...
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Synthesis and Antimicrobial Activity of New Dihydropyrazolo[1,5-a]pyrimidine Derivatives
AbstractObjective: To synthesize new dihydropyrazolo[1,5- a ]pyrimidine derivatives and screen for the antibacterial and antifungal screening. Methods: ...
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Synthesis, biological evaluation and molecular docking studies of novel 1,3,4-thiadiazoles as potential anticancer agents and human carbonic anhydrase inhibitors
Thiosemicarbazide and also 1,3,4-thiadiazole derivatives have been garnering substantial attention from researchers worldwide due to their expansive...
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Fluorinated 2-arylchroman-4-ones and their derivatives: synthesis, structure and antiviral activity
A number of new biologically interesting fluorinated 2-arylchroman-4-ones and their 3-arylidene derivatives were synthesized based on the p -toluenesul...
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Synthesis of (Z)-5-((Substituted-2-(substituted phenyl)-quinoline-3-yl)methylene) Thiazolidinone as Antimicrobial and Anticancer Agent
AbstractA simplistic synthesis of ( Z )-5-((substituted-2-(substituted phenyl)quinolin-3-yl)methylene)-2-thioxothiazolidin-4-one derivatives has been...
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Organohalogen chalcones: design, synthesis, ADMET prediction, molecular dynamics study and inhibition effect on acetylcholinesterase and carbonic anhydrase
In an effort to discover potential acetylcholinesterase (AChE) and carbonic anhydrase (CA) inhibitors, a novel series of organohalogen chalcone...
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The antifungal properties of terpenoids from the endophytic fungus Bipolaris eleusines
A series of terpenoids ( 1–17 ), comprising six new compounds designated bipolariterpenes A-F ( 1–6 ) and eleven recognized compounds ( 7–17 ), were...
