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Design, synthesis and antiproliferative activity of ACY-1215 analogs as potent selective histone deacetylases 6 inhibitors
Design, synthesis and antiproliferative activity of ACY-1215 analogs as potent selective histone deacetylases 6 inhibitors
Histone deacetylase 6 (HDAC6) plays an important role in cancer treatment, and the development of selective HDAC6 inhibito...
Dedication to Dr. Thomas Baillie in recognition of his scientific career
Dedication to Dr. Thomas Baillie in recognition of his scientific career
Professor Thomas Baillie has left a lasting impact on the fie...
Correction: Stable isotope applications in drug development and the elucidation of mechanisms of drug metabolism
Correction: Stable isotope applications in drug development and the elucidation of mechanisms of drug metabolism
Cite this articleTotah, R.A., Rettie, A.E. Correction: Stable isotope applications in drug development and the elucidation...
Synthetic coumarin derivatives with anticoagulation and antiplatelet aggregation inhibitory effects
Synthetic coumarin derivatives with anticoagulation and antiplatelet aggregation inhibitory effects
Thrombosis is the leading cause of illness and mortality worldwide, posing a serious risk to human health and life. Becaus...
Minimizing the DILI potential of carboxylic acid-containing drugs: a perspective
Minimizing the DILI potential of carboxylic acid-containing drugs: a perspective
Drugs containing carboxylic acid moieties are associated with a range of toxicities, some related directly to their pharma...
Synthesis, in-silico based virtual screening,anti-cancer potential of novel1,2,3-triazole-thiadiazole hybrid derivatives as Aurora kinase A (ARK-A) and Extracellular regulated kinase 2 (ERK2) dual inhibitors
Synthesis, in-silico based virtual screening,anti-cancer potential of novel1,2,3-triazole-thiadiazole hybrid derivatives as Aurora kinase A (ARK-A) and Extracellular regulated kinase 2 (ERK2) dual inhibitors
As part of our ongoing efforts to produce promising cytotoxic agents, the novel compounds, 5-(4-(diethylamino)-2-((1-subst...
The metabolic fate of izencitinib, a gut-selective pan-JAK inhibitor, in humans. Identification of unusual fecal metabolites and implications for MIST evaluation
The metabolic fate of izencitinib, a gut-selective pan-JAK inhibitor, in humans. Identification of unusual fecal metabolites and implications for MIST evaluation
Izencitinib is a novel, orally administered pan-JAK inhibitor designed as a gut-selective therapy that was under developme...
Synthesis, in silico, and evaluation of AChE inhibitory activity of N-phthaloylphenylglycine derivatives as potential anti-Alzheimer’s agents
Synthesis, in silico, and evaluation of AChE inhibitory activity of N-phthaloylphenylglycine derivatives as potential anti-Alzheimer’s agents
Mental illnesses are one of the most relevant health problems today, among which Alzheimer’s disease (AD) stands out...
Synthesis, anticancer evaluation and docking studies of novel adamantanyl-1,3,4-oxadiazol hybrid compounds as Aurora-A kinase inhibitors
Synthesis, anticancer evaluation and docking studies of novel adamantanyl-1,3,4-oxadiazol hybrid compounds as Aurora-A kinase inhibitors
Cancer is a devastating disease, but advancements in cancer treatment offer hope for the future. Aurora kinases are a fami...
Bio-evaluation of the 2-nitrochalcones as potential anti-lung cancer agents, inducers of apoptosis and inhibitors of protein kinase (VEGFR-2)
Bio-evaluation of the 2-nitrochalcones as potential anti-lung cancer agents, inducers of apoptosis and inhibitors of protein kinase (VEGFR-2)
A series of the 2-nitrochalcones 3a–3k was synthesized and evaluated for cytotoxicity against the human lung adenoca...
Stable isotope applications in drug development and the elucidation of mechanisms of drug metabolism
Stable isotope applications in drug development and the elucidation of mechanisms of drug metabolism
Over the last 50 years, advances in the production of stable isotopes and mass spectrometry instrumentation have fueled el...
Progress on biphenyl derivatives as PD-1/PD-L1 inhibitors
Progress on biphenyl derivatives as PD-1/PD-L1 inhibitors
Cancer immunotherapy has achieved a leap from the laboratory to the clinic, especially for therapeutic applications based ...
Acyl-CoA thioesters as chemically-reactive intermediates of carboxylic acid-containing drugs
Acyl-CoA thioesters as chemically-reactive intermediates of carboxylic acid-containing drugs
Several carboxylic acid-containing drugs have been withdrawn from clinical use due to adverse drug reactions including idi...
Ester tethered artemisinin-isatin hybrids: design, synthesis and anti-leukemic activity evaluation
Ester tethered artemisinin-isatin hybrids: design, synthesis and anti-leukemic activity evaluation
A series of novel artemisinin-isatin hybrids (7a-t) linked via different lengths of esters were designed, synthesized and ...
Influence of alkyl linkers on the anti-breast cancer activity of dihydroartemisinin-isatin hybrids
Influence of alkyl linkers on the anti-breast cancer activity of dihydroartemisinin-isatin hybrids
To investigate the impact of alkyl linkers of different lengths between dihydroartemisinin and isatin moieties on the anti...
Bioactivity-guided isolation of anti-acetylcholinesterase compounds from Odontites vulgaris Moench
Bioactivity-guided isolation of anti-acetylcholinesterase compounds from Odontites vulgaris Moench
This study aimed to separate the anti-acetylcholinesterase (anti-AChE) compounds from Odontites vulgaris Moench, a member ...
Synthesis of berberine derivatives and their antiviral activity toward respiratory syncytial virus
Synthesis of berberine derivatives and their antiviral activity toward respiratory syncytial virus
A series of derivatives of berberine was synthesized to estimate their antiviral activity toward respiratory syncytial vir...
New tolfenamic acid derivatives with hydrazine-1-carbothioamide and 1,3,4-oxadiazole moieties targeting VEGFR: synthesis, in silico studies, and in vitro anticancer assessment
New tolfenamic acid derivatives with hydrazine-1-carbothioamide and 1,3,4-oxadiazole moieties targeting VEGFR: synthesis, in silico studies, and in vitro anticancer assessment
VEGFR-2 is required for tumor angiogenesis and metastasis. As a cancer therapeutic strategy, blocking VEGFR-2 signaling pa...
The past decade of Genentech experience in elucidation of novel reaction mechanisms in drug metabolism
The past decade of Genentech experience in elucidation of novel reaction mechanisms in drug metabolism
Drug metabolism is critical to many aspects of drug safety and efficacy. Thus, understanding the various intricacies of dr...
Molecular modeling of the phosphoglycerate kinase and fructose-bisphosphate aldolase proteins from Candida glabrata and Candida albicans
Molecular modeling of the phosphoglycerate kinase and fructose-bisphosphate aldolase proteins from Candida glabrata and Candida albicans
Candida species are considered one of the most common fungal pathogens affecting humans. The first colonization stage of t...
Structural and stereochemical determinants for hGAT3 inhibition: development of novel conformationally constrained and substituted analogs of (S)-isoserine
Structural and stereochemical determinants for hGAT3 inhibition: development of novel conformationally constrained and substituted analogs of (S)-isoserine
The GABA transporter 3 (GAT3) is a member of the GABA transporter (GAT) family proposed to have a role in regulating tonic...
A review of the synthesis, bioanalysis, and chemical reactivity of xenobiotic acyl-coenzyme a thioesters
A review of the synthesis, bioanalysis, and chemical reactivity of xenobiotic acyl-coenzyme a thioesters
In this review, we describe current methodologies important for addressing the formation of xenobiotic acyl-coenzyme A-thi...
Structure activity relationship (SAR) driven design and discovery of WCK 5107 (Zidebactam): novel β-lactam enhancer, potent against multidrug-resistant gram-negative pathogens
Structure activity relationship (SAR) driven design and discovery of WCK 5107 (Zidebactam): novel β-lactam enhancer, potent against multidrug-resistant gram-negative pathogens
Extended-spectrum beta-lactamases (ESBL) are the enzymes responsible for producing multidrug-resistant (MDR) bacterial str...
Synthesis of indole-based ferulic acid derivatives and in vitro evaluation of antiviral activity against SARS-CoV-2
Synthesis of indole-based ferulic acid derivatives and in vitro evaluation of antiviral activity against SARS-CoV-2
The search for an effective small molecule against the severe acute respiratory syndrome related coronavirus 2 (SARS-CoV-2...
A review of the mechanisms of valproate-induced liver injury with an emphasis on the role of reactive metabolites discovered by Tom Baillie
A review of the mechanisms of valproate-induced liver injury with an emphasis on the role of reactive metabolites discovered by Tom Baillie
The anticonvulsant valproic acid (VA) is associated with a range of idiosyncratic drug reactions; the most common is liver...
Synthesis of 2-amino-4H-chromenes catalyst-free via sequential Knoevenagel-Michael reaction and evaluation of biological activity in tumor cells
Synthesis of 2-amino-4H-chromenes catalyst-free via sequential Knoevenagel-Michael reaction and evaluation of biological activity in tumor cells
This work focuses on investigating solvents for the catalyst-free synthesis of 2-amino-4H-chromenes from salicylaldehydes ...
Synthesis of amide warhead containing coumarin derivatives as potential pancreatic lipase inhibitors: in silico and in vitro evaluation for obesity treatment
Synthesis of amide warhead containing coumarin derivatives as potential pancreatic lipase inhibitors: in silico and in vitro evaluation for obesity treatment
A series of coumarin-3-carboxamide analogues has been designed, synthesized and assessed for their ability to inhibit panc...
Glutathione and glutathione disulfide – their biomedical and pharmaceutical applications
Glutathione and glutathione disulfide – their biomedical and pharmaceutical applications
Glutathione (GSH) is an endogenous tripeptide (Glu-Cys-Gly) and the most abundant endogenous antioxidant. It protects the ...
Discovery of deguelin derivatives in combination with fluconazole against drug-resistant Candida albicans
Discovery of deguelin derivatives in combination with fluconazole against drug-resistant Candida albicans
Candida albicans, as the most prevalent opportunistic pathogenic fungus, has caused great difficulty in its clinical manag...
Direct syntheses of stereoisomers of 3-fluoro GABA and β-fluoroamine analogues of the calcium receptor (CaR) agonists, cinacalcet, tecalcet, fendiline and NPS R-467
Direct syntheses of stereoisomers of 3-fluoro GABA and β-fluoroamine analogues of the calcium receptor (CaR) agonists, cinacalcet, tecalcet, fendiline and NPS R-467
Synthetic routes following a sequential MacMillan organocatalytic asymmetric α-fluorination protocol for aldehydes an...
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