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Exploring novel anticancer pyrazole benzenesulfonamides featuring tail approach strategy as carbonic anhydrase inhibitors
Exploring novel anticancer pyrazole benzenesulfonamides featuring tail approach strategy as carbonic anhydrase inhibitors
Carbonic anhydrases (CAs) are essential metalloenzymes, present in both prokaryotes and eukaryotes, that catalyse the reve...
Synthesis and evaluation of aromatic BDSF bioisosteres on biofilm formation and colistin sensitivity in pathogenic bacteria
Synthesis and evaluation of aromatic BDSF bioisosteres on biofilm formation and colistin sensitivity in pathogenic bacteria
KeywordsDiffusible signal factorQuorum sensingBiofilmsResistanceAcinetobacter baumanniiEscherichia coliBurkholderia multiv...
Development of a NIR fluorescent probe for fluorescence-assisted EGFR-TKI applicable patients screening and drug resistance monitoring
Development of a NIR fluorescent probe for fluorescence-assisted EGFR-TKI applicable patients screening and drug resistance monitoring
Lung cancer reminds one of the most lethal and highest morbidity cancer worldwide, and non-small cell lung cancer (NSCLC) ...
Synthesis, cytotoxic activity evaluation and mechanistic investigation of novel 3,7-diarylsubstituted 6-azaindoles
Synthesis, cytotoxic activity evaluation and mechanistic investigation of novel 3,7-diarylsubstituted 6-azaindoles
All four positional isomers of the azaindole (1H-pyrrolopyridine) fused ring system can be considered as isosteric structu...
Synthesis and biological evaluation of fluoroquinolones containing a pyridoxine derivatives moiety
Synthesis and biological evaluation of fluoroquinolones containing a pyridoxine derivatives moiety
Nowadays, the increasing emergence of antibiotic resistance in pathogenic bacteria is one of the biggest problems of the h...
Galantamine-memantine hybrids for Alzheimer's disease: The influence of linker rigidity in biological activity and pharmacokinetic properties
Galantamine-memantine hybrids for Alzheimer's disease: The influence of linker rigidity in biological activity and pharmacokinetic properties
Neurodegenerative processes characterizing Alzheimer's disease (AD) are strictly related to the impairment of cholinergic ...
Targeting protein kinases for the treatment of Alzheimer's disease: Recent progress and future perspectives
Targeting protein kinases for the treatment of Alzheimer's disease: Recent progress and future perspectives
Alzheimer's disease (AD), the most common neurodegenerative disease, was first described by German psychiatrist Alos Alzhe...
A dipyridophenazine Ni(II) dithiolene complex as a dual-acting cancer phototherapy agent activatable within the phototherapeutic window
A dipyridophenazine Ni(II) dithiolene complex as a dual-acting cancer phototherapy agent activatable within the phototherapeutic window
Photoactive transition metal complexes that offer a multimodal approach to cancer treatment are of considerable significan...
Discovery of 1,2-diaryl-3-oxopyrazolidin-4-carboxamides as a new class of MurA enzyme inhibitors and characterization of their antibacterial activity
Discovery of 1,2-diaryl-3-oxopyrazolidin-4-carboxamides as a new class of MurA enzyme inhibitors and characterization of their antibacterial activity
The persistent emergence of multidrug-resistant bacterial strains poses an enormous threat to the global public health, je...
Design, synthesis, and anti-respiratory syncytial virus potential of novel 3-(1,2,3-triazol-1-yl)furoxazine-fused benzimidazole derivatives
Design, synthesis, and anti-respiratory syncytial virus potential of novel 3-(1,2,3-triazol-1-yl)furoxazine-fused benzimidazole derivatives
Human respiratory syncytial virus (RSV) is a negative-sense enveloped RNA virus belonging to the family Paramyxoviridae an...
Progress in the development of TRPV1 small-molecule antagonists: Novel Strategies for pain management
Progress in the development of TRPV1 small-molecule antagonists: Novel Strategies for pain management
Pain management represents a global challenge. Pain arising from various causes, such as trauma, disease, surgery, chemoth...
Applications of oxetanes in drug discovery and medicinal chemistry
Applications of oxetanes in drug discovery and medicinal chemistry
Oxetane is an oxygen-containing four-membered heterocycle, which exhibits significant strain energy (c.a. 106 kJ mol−1) [1...
Fragment-based and structure-guided discovery of perforin inhibitors
Fragment-based and structure-guided discovery of perforin inhibitors
Perforin is a pore-forming protein whose normal function enables cytotoxic T and natural killer (NK) cells to kill virus-i...
Design, synthesis and antitrypanosomatid activity of 2-nitroimidazole-3,5-disubstituted isoxazole compounds based on benznidazole
Design, synthesis and antitrypanosomatid activity of 2-nitroimidazole-3,5-disubstituted isoxazole compounds based on benznidazole
According to Drugs for Neglected Diseases initiative (DNDi) “It all starts with a compound library.” The drug discovery pr...
Current advances and development strategies of orally bioavailable PROTACs
Current advances and development strategies of orally bioavailable PROTACs
Target protein degradation (TPD) is a promising therapeutic strategy for disease treatment. Proteolysis-targeting chimera ...
Technologies of targeting histone deacetylase in drug discovery: Current progress and emerging prospects
Technologies of targeting histone deacetylase in drug discovery: Current progress and emerging prospects
The post-translational modification (PTM) process of histones can modulate changes in chromatin machinery to participate i...
The latest perspectives of small molecules FMS kinase inhibitors
The latest perspectives of small molecules FMS kinase inhibitors
FMS kinase, also known as c-FMS, CSF-1R, M-CSFR, and CD115, is a type III tyrosine kinase receptor (TKR) that belongs to t...
Synthesis and mechanism of action of new purine derivatives against triple negative breast cancer
Synthesis and mechanism of action of new purine derivatives against triple negative breast cancer
The International Agency for Research on Cancer released the latest data showing that breast cancer has surpassed lung can...
Synthesis of bitopic ligands based on fallypride and evaluation of their affinity and selectivity towards dopamine D2 and D3 receptors
Synthesis of bitopic ligands based on fallypride and evaluation of their affinity and selectivity towards dopamine D2 and D3 receptors
The dopamine 2-like receptors belong to the G-protein-coupled receptors (GPCRs). Various neurological and neuropsychiatric...
Identification of novel dithiocarbamate-copper complexes targeting p97/NPL4 pathway in cancer cells
Identification of novel dithiocarbamate-copper complexes targeting p97/NPL4 pathway in cancer cells
Drug repurposing became an exciting strategy for finding new oncological drugs [1]. One such candidate is the long-term ap...
Novel chlorin e6-based conjugates of tyrosine kinase inhibitors: Synthesis and photobiological evaluation as potent photosensitizers for photodynamic therapy
Novel chlorin e6-based conjugates of tyrosine kinase inhibitors: Synthesis and photobiological evaluation as potent photosensitizers for photodynamic therapy
Photodynamic therapy (PDT) has been a clinically approved therapeutic modality for efficient treatment of various oncologi...
The design, synthesis, and inhibition of Clostridioides difficile spore germination by acyclic and bicyclic tertiary amide analogs of cholate
The design, synthesis, and inhibition of Clostridioides difficile spore germination by acyclic and bicyclic tertiary amide analogs of cholate
Clostridioides difficile is an anaerobic bacterium that can colonize the gastrointestinal tract and cause severe and poten...
Design, synthesis and evaluation of ursodeoxycholic acid-cinnamic acid hybrids as potential anti-inflammatory agents by inhibiting Akt/NF-κB and MAPK signaling pathways
Design, synthesis and evaluation of ursodeoxycholic acid-cinnamic acid hybrids as potential anti-inflammatory agents by inhibiting Akt/NF-κB and MAPK signaling pathways
Inflammation is the physiological immune response to infectious pathogens or injuries and its main role is to eliminate ha...
Discovery of novel benzofuran-based derivatives as acetylcholinesterase inhibitors for the treatment of Alzheimer's disease: Design, synthesis, biological evaluation, molecular docking and 3D-QSAR investigation
Discovery of novel benzofuran-based derivatives as acetylcholinesterase inhibitors for the treatment of Alzheimer's disease: Design, synthesis, biological evaluation, molecular docking and 3D-QSAR investigation
Alzheimer's disease (AD) is a chronic, irreversible neurodegenerative disorder of the central nervous system that causes p...
Recent advances in small molecule and peptide inhibitors of glucose-regulated protein 78 for cancer therapy
Recent advances in small molecule and peptide inhibitors of glucose-regulated protein 78 for cancer therapy
The 70-kDa heat shock protein 70 (Hsp70) family is a class of highly conserved chaperones that play a central role in prot...
Identification of 1,3,4-oxadiazolyl-containing β-carboline derivatives as novel α-glucosidase inhibitors with antidiabetic activity
Identification of 1,3,4-oxadiazolyl-containing β-carboline derivatives as novel α-glucosidase inhibitors with antidiabetic activity
Diabetes mellitus (DM) is a chronic metabolic disease characterized by high levels of blood glucose [1,2]. Long-term uncon...
Discovery of a novel series of potent carbonic anhydrase inhibitors with selective affinity for μ Opioid receptor for Safer and long-lasting analgesia
Discovery of a novel series of potent carbonic anhydrase inhibitors with selective affinity for μ Opioid receptor for Safer and long-lasting analgesia
Opioids, such as morphine and fentanyl, are a mainstay of pain management and the analgesic of choice for the relief of mo...
Rapid access to icetexane diterpenes: Their protective effects against lipopolysaccharides-induced acute lung injury via PI3K/AKT/NF-κB axis in macrophages
Rapid access to icetexane diterpenes: Their protective effects against lipopolysaccharides-induced acute lung injury via PI3K/AKT/NF-κB axis in macrophages
Acute lung injury (ALI)/acute respiratory distress syndrome (ARDS) represents a challenging clinical syndrome that leads t...
Discovery of Pyrazolo[1,5-a]pyrimidine derivative as a potent and selective PI3Kγ/δ dual inhibitor
Discovery of Pyrazolo[1,5-a]pyrimidine derivative as a potent and selective PI3Kγ/δ dual inhibitor
Phosphoinositide-3 kinases (PI3Ks) are key cellular signaling proteins involved in cell proliferation, growth, differentia...
Discovery of NLRP3 inhibitors using machine learning: Identification of a hit compound to treat NLRP3 activation-driven diseases
Discovery of NLRP3 inhibitors using machine learning: Identification of a hit compound to treat NLRP3 activation-driven diseases
The innate immune response is one of the key means by which mammals recognize the infection and initiate the process of pa...
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