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Characterization of the CO release properties of a common CO donor, CORM-401, in the context of its application in studying CO biology
Characterization of the CO release properties of a common CO donor, CORM-401, in the context of its application in studying CO biology
In studying CO for its pathophysiological roles, four metal/borane-carbonyl complexes have been widely used as CO-releasin...
Antitumor studies on celastrol and its derivatives as RORα agonists and RORγ inhibitors based on Alphafold reverse docking strategy
Antitumor studies on celastrol and its derivatives as RORα agonists and RORγ inhibitors based on Alphafold reverse docking strategy
Celastrol (CSL), an active compound extracted from the root bark of Tripterygium wilfordii, has been studied for its outst...
Phenoxyalkyl cyclic and acyclic amine derivatives: what do they teach us about scaffold-based drug design?
Phenoxyalkyl cyclic and acyclic amine derivatives: what do they teach us about scaffold-based drug design?
Fragment-based drug design of new bioactive scaffolds is a recent aspect of medicinal chemistry that provides a faster and...
Synthesis and anticancer activity of novel coumarin-stilbene hybrids with different hydrocarbon chains as linkers
Synthesis and anticancer activity of novel coumarin-stilbene hybrids with different hydrocarbon chains as linkers
Stilbene derivatives (pterostilbene and resveratrol) and 4-methylumbelliferone occur naturally in plants. These compounds ...
Vital residues-orientated rational design of butenolide inhibitors targeting Of ChtI
Vital residues-orientated rational design of butenolide inhibitors targeting Of ChtI
An effective approach for discovering small molecular inhibitors is the residues-oriented strategy based on enzyme analysi...
Design, synthesis, and in vitro biological evaluation of novel HDAC inhibitors bearing C-1 phenyl substituted tetrahydroisoquinoline Cap moiety as anti-tumor therapeutic agents
Design, synthesis, and in vitro biological evaluation of novel HDAC inhibitors bearing C-1 phenyl substituted tetrahydroisoquinoline Cap moiety as anti-tumor therapeutic agents
Herein, a structurally novel class of histone deacetylase (HDAC) inhibitors featuring the C-1 phenyl substituted tetrahydr...
Design, synthesis and antitumor activity evaluation of novel benzamide HDAC inhibitors
Design, synthesis and antitumor activity evaluation of novel benzamide HDAC inhibitors
In recent years, histone deacetylase (HDAC) has become one of the hottest and most effective targets for the treatment of ...
Diffractaic acid and its ethers as anti-respiratory syncytial virus agents
Diffractaic acid and its ethers as anti-respiratory syncytial virus agents
A major secondary metabolite of lichens, diffractaic acid, was found here to exert a significant antiviral action on respi...
Synthesis, urease inhibitory and anticancer evaluation of glucosamine-sulfonylurea conjugates
Synthesis, urease inhibitory and anticancer evaluation of glucosamine-sulfonylurea conjugates
Urease catalyses the hydrolysis of urea to ammonia and carbon dioxide. This enzyme is important in the virulence of severa...
Motor and non-motor symptoms, drugs, and their mode of action in Parkinson’s disease (PD): a review
Motor and non-motor symptoms, drugs, and their mode of action in Parkinson’s disease (PD): a review
Parkinson’s disease is second most common neurodegenerative disorder neurological illness that primarily affects pat...
Bioassay-guided fractionations of Cannabis sativa extract and HPLC-assisted purifications of anti-proliferative active fractions lead to the isolation of 16 known and one new phytomolecule and their in-silico analysis
Bioassay-guided fractionations of Cannabis sativa extract and HPLC-assisted purifications of anti-proliferative active fractions lead to the isolation of 16 known and one new phytomolecule and their in-silico analysis
The comprehensive anti-cancer activities of cannabinoid acids and non-cannabinoids are not fully explored. Herein we repor...
Design, synthesis, and biochemical and computational screening of novel oxindole derivatives as inhibitors of Aurora A kinase and SARS-CoV-2 spike/host ACE2 interaction
Design, synthesis, and biochemical and computational screening of novel oxindole derivatives as inhibitors of Aurora A kinase and SARS-CoV-2 spike/host ACE2 interaction
Isatin (indol-2,3-dione), a secondary metabolite of tryptophan, has been used as the core structure to design several comp...
Evaluation of ortho-substituted Bis-Functionalized Triazoles as Tyrosinase Inhibitors: Modulating Dopamine Synthesis and Behavior in Zebrafish
Evaluation of ortho-substituted Bis-Functionalized Triazoles as Tyrosinase Inhibitors: Modulating Dopamine Synthesis and Behavior in Zebrafish
Facile and green chemistry pathways are utilized through microwave-assisted organic synthesis (MAOS) to generate biologica...
Adenine derivatives as inhibitors of the casein kinase CK1delta enzyme
Adenine derivatives as inhibitors of the casein kinase CK1delta enzyme
Overexpression of CK1δ has been associated to the development of cancer and neurodegenerative disorders, making ligan...
Evolution and challenges of opioids in pain management: Understanding mechanisms and exploring strategies for safer analgesics
Evolution and challenges of opioids in pain management: Understanding mechanisms and exploring strategies for safer analgesics
Opioids traced back to ancient civilizations, have evolved in their usage for acute and chronic pain treatment. Their inte...
Development of novel chalcone derivatives as multifunctional agents for the treatment of Alzheimer’s disease
Development of novel chalcone derivatives as multifunctional agents for the treatment of Alzheimer’s disease
To develop multifunctional agents for the treatment of Alzheimer’s disease (AD), a series of novel chalcone derivati...
2-Styrylchromones as inhibitors of α-amylase and α-glucosidase enzymes for the management of type 2 diabetes mellitus
2-Styrylchromones as inhibitors of α-amylase and α-glucosidase enzymes for the management of type 2 diabetes mellitus
α-amylase and α-glucosidase are key enzymes implicated in carbohydrate digestion and their inhibition has been s...
Insights on synthetic strategies and structure-activity relationship of donepezil and its derivatives
Insights on synthetic strategies and structure-activity relationship of donepezil and its derivatives
This comprehensive review focuses on the synthesis and derivatives of donepezil, a pivotal Alzheimer’s disease (AD) ...
Preliminary structure−activity relationships analysis on N-(3,5-dichlorophenyl)-4,5-dihydronaphtho[1,2-d]thiazol-2-amine, a disruptor of mycobacterial energetics
Preliminary structure−activity relationships analysis on N-(3,5-dichlorophenyl)-4,5-dihydronaphtho[1,2-d]thiazol-2-amine, a disruptor of mycobacterial energetics
The increasing emergence of drug-resistance among mycobacteria represents a serious global health threat, requiring novel ...
Targeting disease with benzoxazoles: a comprehensive review of recent developments
Targeting disease with benzoxazoles: a comprehensive review of recent developments
Benzoxazole is an attractive scaffold in medicinal chemistry due to its diverse biological applications. From 2016 to 2023...
Synthesis, characterization, and anticancer activity of syringaldehyde-derived chalcones against female cancers
Synthesis, characterization, and anticancer activity of syringaldehyde-derived chalcones against female cancers
A series of novel chalcone analogs derived from syringaldehyde have been synthesized through acid or base-catalyzed aldol ...
The use of single-molecule FRET for the characterization of Holliday junctions containing human telomeric DNA: a methodological approach for nanoscale distance, mobility, and stability measurements
The use of single-molecule FRET for the characterization of Holliday junctions containing human telomeric DNA: a methodological approach for nanoscale distance, mobility, and stability measurements
Single-molecule analysis has emerged as a powerful biophysical technique, allowing the investigation of molecular interact...
Synthesis and pharmacological activities of Schiff bases with some transition metal complexes: a review
Synthesis and pharmacological activities of Schiff bases with some transition metal complexes: a review
Schiff bases transition metal complexes have received significant attentions in the scientific community for their versati...
Identification of novel benzoyl hydrazine derivatives as activators of neddylation pathway to inhibit the tumor progression in vitro
Identification of novel benzoyl hydrazine derivatives as activators of neddylation pathway to inhibit the tumor progression in vitro
Neddylation modification is frequently overexpressed in many types of human tumors. As a result, targeting neddylation pat...
Benzocaine-N-acylindoline conjugates: synthesis and antiviral activity against Coxsackievirus B3
Benzocaine-N-acylindoline conjugates: synthesis and antiviral activity against Coxsackievirus B3
Indoline-5-sulfonamide derivatives of benzocaine have been synthesized using a sequence of three reactions: N-acylation, s...
Novel biologically active pyridine derivatives: Synthesis, structure characterization, in vitro antimicrobial evaluation and structure-activity relationship
Novel biologically active pyridine derivatives: Synthesis, structure characterization, in vitro antimicrobial evaluation and structure-activity relationship
The rate of microbial resistance has continued to rise significantly as the availability of new antibiotics has declined. ...
Selectivity of N(2)-substituted oxotriazinoindole aldose reductase inhibitors is determined by the interaction pattern with Pro301-Arg312 loop of aldehyde reductase
Selectivity of N(2)-substituted oxotriazinoindole aldose reductase inhibitors is determined by the interaction pattern with Pro301-Arg312 loop of aldehyde reductase
Novel oxotriazinoindoles (OTIs) were recently reported as highly efficient and selective aldose reductase inhibitors. Here...
Exploring the latest breakthroughs in rhodesain inhibitors for African trypanosomiasis
Exploring the latest breakthroughs in rhodesain inhibitors for African trypanosomiasis
Human African Trypanosomiasis is a serious public health concern, and new chemical therapeutic agents need to be developed...
Unveiling the potential of prodrug and drug-conjugate strategies in treatment of diabetes mellitus and its complications
Unveiling the potential of prodrug and drug-conjugate strategies in treatment of diabetes mellitus and its complications
The 2021 statistics from the International Diabetes Federation reveals that approximately 537 million adults between the a...
Identification of α-mangostin as a potent inhibitor of β-lactamase OXA-48
Identification of α-mangostin as a potent inhibitor of β-lactamase OXA-48
The production of carbapenemases is a significant mechanism contributing to carbapenem resistance in Enterobacteriaceae. A...
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