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Development, preclinical evaluation and preliminary dosimetry profiling of SB03178, a first-of-its-kind benzo[h]quinoline-based fibroblast activation protein-α-targeted radiotheranostic for cancer imaging and therapy
Development, preclinical evaluation and preliminary dosimetry profiling of SB03178, a first-of-its-kind benzo[h]quinoline-based fibroblast activation protein-α-targeted radiotheranostic for cancer imaging and therapy
Fibroblast activation protein-α (FAP) is a transmembrane glycoprotein that is restrictively expressed on normal fibroblast...
Does size matter? – Comparing pyranoses with septanoses as ligands of the bacterial lectin FimH
Does size matter? – Comparing pyranoses with septanoses as ligands of the bacterial lectin FimH
Many biological surfaces are densely covered with a layer of carbohydrates, the so-called glycocalyx [1]. Recognition of t...
Identification of the exosomal PD-L1 inhibitor to promote the PD-1 targeting therapy of gastric cancer
Identification of the exosomal PD-L1 inhibitor to promote the PD-1 targeting therapy of gastric cancer
Programmed death 1/programmed death-ligand 1 (PD-1/PD-L1) targeting therapy is a key strategy in gastric cancer treatment,...
Pyrazolamide derivatives inhibit α-Synuclein aggregation, disaggregate preformed fibers, and reduce inclusion formation in neuron cells
Pyrazolamide derivatives inhibit α-Synuclein aggregation, disaggregate preformed fibers, and reduce inclusion formation in neuron cells
Parkinson's disease (PD) is characterized by the loss of dopaminergic neurons in the substantia nigra and the presence of ...
Discovery of the novel and potent histamine H1 receptor antagonists for treatment of allergic diseases
Discovery of the novel and potent histamine H1 receptor antagonists for treatment of allergic diseases
Allergic diseases are caused by the body's abnormal immune response to allergens, including acute and chronic urticaria, c...
Novel aminothiazoximone-corbelled ethoxycarbonylpyrimidones with antibiofilm activity to conquer Gram-negative bacteria through potential multitargeting effects
Novel aminothiazoximone-corbelled ethoxycarbonylpyrimidones with antibiofilm activity to conquer Gram-negative bacteria through potential multitargeting effects
Bacterial resistance to available antibiotics has resulted in limited options for treatment of patients suffering from lif...
Design, synthesis and biological evaluation of novel 1,2,4a,5-tetrahydro-4H-benzo[b][1,4]oxazino[4,3-d][1,4]oxazine-based AAK1 inhibitors with anti-viral property against SARS-CoV-2
Design, synthesis and biological evaluation of novel 1,2,4a,5-tetrahydro-4H-benzo[b][1,4]oxazino[4,3-d][1,4]oxazine-based AAK1 inhibitors with anti-viral property against SARS-CoV-2
The coronavirus disease 2019 (COVID-19) pandemic caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) ha...
Design, synthesis, biological evaluation and in silico studies of novel quinoline derivatives as potential radioprotective molecules targeting the TLR2 and p53 pathways
Design, synthesis, biological evaluation and in silico studies of novel quinoline derivatives as potential radioprotective molecules targeting the TLR2 and p53 pathways
Exposure to a high dose of ionizing radiation (IR) can cause dysfunction in functional systems [1], and damage to the dige...
Carbazole to indolazepinone scaffold morphing leads to potent cell-active dengue antivirals
Carbazole to indolazepinone scaffold morphing leads to potent cell-active dengue antivirals
According to WHO, dengue virus is classed among major threats for future pandemics and remains at large an unmet medical n...
Design, synthesis and biological evaluation of thiazolyl-halogenated pyrroles or pyrazoles as novel antibacterial and antibiofilm agents
Design, synthesis and biological evaluation of thiazolyl-halogenated pyrroles or pyrazoles as novel antibacterial and antibiofilm agents
The emergence of drug-resistant bacteria leading to difficult-to-control infections is a major threat to human life and ha...
Structural modification based on the diclofenac scaffold: Achieving reduced colitis side effects through COX-2/NLRP3 selective inhibition
Structural modification based on the diclofenac scaffold: Achieving reduced colitis side effects through COX-2/NLRP3 selective inhibition
Ulcerative colitis is a chronic inflammatory bowel disease of multifactorial origin. The global incidence of UC is progres...
Identification of 3-aryl-5-methyl-isoxazole-4-carboxamide derivatives and analogs as novel HIF-2α agonists through docking-based virtual screening and structural modification
Identification of 3-aryl-5-methyl-isoxazole-4-carboxamide derivatives and analogs as novel HIF-2α agonists through docking-based virtual screening and structural modification
Hypoxia-inducible factors (HIFs) are members of the basic helix loop-helix PER-ARNT-SIM (bHLH-PAS) family of transcription...
The antibacterial properties of branched peptides based on poly(l-arginine): In vitro antibacterial evaluation and molecular dynamic simulations
The antibacterial properties of branched peptides based on poly(l-arginine): In vitro antibacterial evaluation and molecular dynamic simulations
Health-care associated infections (HAIs) are a major issue in the medical field. Indeed, according to Centers for Disease ...
Discovery of FLT3-targeting PROTACs with potent antiproliferative activity against acute myeloid leukemia cells harboring FLT3 mutations
Discovery of FLT3-targeting PROTACs with potent antiproliferative activity against acute myeloid leukemia cells harboring FLT3 mutations
Acute myeloid leukemia (AML) is a hematopoietic malignancy characterized by strong invasiveness, poor prognosis, high recu...
Thiadiazole-, selenadiazole- and triazole-fused anthraquinones as G-quadruplex targeting anticancer compounds
Thiadiazole-, selenadiazole- and triazole-fused anthraquinones as G-quadruplex targeting anticancer compounds
Nucleic acids are important targets for many antitumor drugs [1,2]. They are of particular significance in the medicinal c...
Rare flavanone-diarylheptanoid hybrids from Typha angustifolia shows anti breast cancer activity via activating TGF-β1/Smad signaling pathway
Rare flavanone-diarylheptanoid hybrids from Typha angustifolia shows anti breast cancer activity via activating TGF-β1/Smad signaling pathway
Calyxins represent a rare class of natural products hybridized from a diarylheptanoid and a flavonoid (chalcone or flavano...
Design, synthesis, and biological evaluation of first-in-class indomethacin-based PROTACs degrading SARS-CoV-2 main protease and with broad-spectrum antiviral activity
Design, synthesis, and biological evaluation of first-in-class indomethacin-based PROTACs degrading SARS-CoV-2 main protease and with broad-spectrum antiviral activity
To date, Proteolysis Targeting Chimera (PROTAC) technology has been successfully applied to mediate proteasomal-induced de...
Novel aroyl guanidine anti-trypanosomal compounds that exert opposing effects on parasite energy metabolism
Novel aroyl guanidine anti-trypanosomal compounds that exert opposing effects on parasite energy metabolism
Human African trypanosomiasis (HAT), or sleeping sickness, is a neglected tropical disease with current treatments marred ...
Discovery of N-(5-amido-2-methylphenyl)-5-methylisoxazole-3-carboxamide as dual CSF-1R/c-Kit Inhibitors with improved stability and BBB permeability
Discovery of N-(5-amido-2-methylphenyl)-5-methylisoxazole-3-carboxamide as dual CSF-1R/c-Kit Inhibitors with improved stability and BBB permeability
The discovery of CSF-1R kinase [1] as a tumor gene implicated in Feline McDonough sarcoma [2] marked the identification of...
Novel sulfonamide-indolinone hybrids targeting mitochondrial respiration of breast cancer cells
Novel sulfonamide-indolinone hybrids targeting mitochondrial respiration of breast cancer cells
Breast cancer, the so-called pink killer, is one of the major causes of death in women worldwide [1]. With a continuously ...
Discovery and exploration of novel somatostatin receptor subtype 5 (SSTR5) antagonists for the treatment of cholesterol gallstones
Discovery and exploration of novel somatostatin receptor subtype 5 (SSTR5) antagonists for the treatment of cholesterol gallstones
Cholesterol gallstones are a gastrointestinal disease characterized by chronic, recurrent, high incidence rate (∼15%–20 %)...
Design, synthesis and evaluation of novel deferasirox derivatives with high antifungal potency in vitro and in vivo
Design, synthesis and evaluation of novel deferasirox derivatives with high antifungal potency in vitro and in vivo
Invasive fungal infections (IFIs) are an increasing global public health concern, particularly affecting people with under...
Whole cell hydride Meisenheimer complex biotransformation guided optimization of antimycobacterial benzothiazinones
Whole cell hydride Meisenheimer complex biotransformation guided optimization of antimycobacterial benzothiazinones
Tuberculosis (TB) is caused by Mycobacterium tuberculosis and is a major threat to global health. With an estimated 10.6 m...
Investigating the anti-cancer potential of pyrimethamine analogues through a modern chemical biology lens
Investigating the anti-cancer potential of pyrimethamine analogues through a modern chemical biology lens
Dihydrofolate reductase (DHFR) is responsible for catalyzing the reduction of folate and dihydrofolate (DHF) into tetrahyd...
Structure-based design of SARS-CoV-2 papain-like protease inhibitors
Structure-based design of SARS-CoV-2 papain-like protease inhibitors
It has been almost four years since the beginning of the COVID-19 pandemic. The COVID-19 pandemic is caused by SARS-CoV-2,...
Design and synthesis of dual BRD4/Src inhibitors for treatment of triple-negative breast cancer
Design and synthesis of dual BRD4/Src inhibitors for treatment of triple-negative breast cancer
Target-based drug discovery (TDD) has been the primary approach leveraged by the pharmaceutical industry in recent decades...
An imidazo[1,2-a]pyridine-pyridine derivative potently inhibits FLT3-ITD and FLT3-ITD secondary mutants, including gilteritinib-resistant FLT3-ITD/F691L
An imidazo[1,2-a]pyridine-pyridine derivative potently inhibits FLT3-ITD and FLT3-ITD secondary mutants, including gilteritinib-resistant FLT3-ITD/F691L
Gain-of-function mutations in FMS-like tyrosine kinase 3 (FLT3) are detected in approximately 30 % of newly diagnosed acut...
Design, synthesis, and biological evaluation of 2-amino-6-methyl-phenol derivatives targeting lipid peroxidation with potent anti-ferroptotic activities
Design, synthesis, and biological evaluation of 2-amino-6-methyl-phenol derivatives targeting lipid peroxidation with potent anti-ferroptotic activities
Ferroptosis is a form of regulated cell death characterized by the iron-dependent accumulation of lipid hydroperoxides to ...
Brazilin-7-acetate, a novel potential drug of Parkinson's disease, hinders the formation of α-synuclein fibril, mitigates cytotoxicity, and decreases oxidative stress
Brazilin-7-acetate, a novel potential drug of Parkinson's disease, hinders the formation of α-synuclein fibril, mitigates cytotoxicity, and decreases oxidative stress
Parkinson's disease (PD) is the second most common neurodegenerative disorder. According to the statistics of the World Pa...
Novel antimicrobial peptides modified with fluorinated sulfono-γ-AA having high stability and targeting multidrug-resistant bacteria infections
Novel antimicrobial peptides modified with fluorinated sulfono-γ-AA having high stability and targeting multidrug-resistant bacteria infections
Multidrug-resistant (MDR) ESKAPE pathogens have emerged as a serious global public health threat due to the abuse of antib...
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