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Small molecular inhibitors targeting Janus kinases (JAKs) for the treatment of psoriasis
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Orphan GPCRs regulate the metabolic liver diseases through mediating the crosstalk between the liver and immune cells: Mechanisms and therapeutics
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Targeting p53 activation: Recent therapeutic advances in cancer and diabetic macular edema
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Recent advances in functional activatable probes for oncological surgery: Illuminating precision or hindering clinical translation?
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Discovery of thiazolylcyanovinyl benzopyridone acids: Potential new generation antibacterial oxacins?
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Discovery of novel hydrazinyl thiazole derivatives as potent anticancer agents by inhibiting eIF4E/eIF4G interactions
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Discovery of novel fluorescent amino-pyrazolines that detect and kill Mycobacterium tuberculosis
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Synthesis and evaluation of new 5-(1H-1,2,4-triazol-3-yl)-1,2,4-oxadiazole derivatives and their application as OXPHOS inhibitors
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Targeting dihydroorotate dehydrogenase (DHODH) for host-directed therapy: Discovery of a novel alkyne-based scaffold inhibitor effective against SARS-CoV-2
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Lead optimization of a CHI3L1 inhibitor for Glioblastoma: Enhanced target engagement, pharmacokinetics, and efficacy in 3D spheroid models
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Discovery of novel thiazolylhydrazone derivatives as potent anti-cancer agents inducing ferroptosis via direct NRF2 inhibition
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Synthesis and evaluation of lactam and maleimide derivatives of 16-hydroxycleroda-3, 13 (14) Z-dien-15, 16-olide from Polyalthia longifolia as potential anticancer agents
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Discovery of a novel Genipin derivative targeting YB-1 to enhance the P-glycoprotein-mediated paclitaxel sensitivity of paclitaxel-resistant non-small cell lung cancer
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1,3-Thiazole nucleus as promising molecular platform against antimicrobial resistance: a recent overview in drug discovery
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Discovery of SA-8 as a potent SHP2-AUTAC degrader in cancer therapy
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Recent advance of hypoxia-inducible factor prolyl hydroxylases inhibitors for anemia therapy
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Local enhancement of cationic charge density via polyamine side chain incorporation improves the selectivity of antimicrobial peptoids
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Design and synthesis of Riluzole-Ciprofloxacin hybrids as selective MST3 inhibitors for cancer treatment
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Highly potent dipeptidyl peptidase 8/9 (DPP8/9) inhibitors designed via relative binding free energy calculations
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Discovery of 3,4-dihydroisoquinoline-2(1H)-carboxamide STING inhibitors as anti-inflammatory agents
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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...
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