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Discovery of novel rigid STING PROTAC degraders as potential therapeutics for acute kidney injury
Acute Kidney Injury (AKI) refers to a disease of rapid deterioration of renal function characterized by acute inflammation...
Discovery of novel azetidine-based imidazopyridines as selective and orally bioavailable inhibitors of phosphodiesterase 10A for the treatment of pulmonary arterial hypertension
Pulmonary arterial hypertension (PAH), a progressive and life-threatening disease classified as a subtype of pulmonary hyp...
Structural simplification of quaternary benzophenanthridine alkaloids generating a candidate for the treatment of non-small cell lung cancer
Natural products and their derivatives represent a significant source of therapeutic agents, playing a crucial role in the...
Tetracationic tetraaryltetranaphtho[2,3]porphyrins for photodynamic inactivation against Staphylococcus aureus biofilm
Infectious diseases continue to pose one of the most significant challenges to global healthcare. Traditionally, antibioti...
Discovery of ultra short β-peptoids with selective activity against drug-resistant Mycobacterium tuberculosis
The search for new antibiotics against drug-resistant microbes has led to renewed focus on antimicrobial peptides (AMPs) a...
Exploring Si-phthalocyanines with different valency for PSMA-targeted photodynamic therapy: Synthesis and preclinical validation
Prostate cancer remains a significant health concern, with existing treatments often proving invasive or inadequate in pre...
A highly active angiotensin I-converting enzyme inhibitory peptide KAKW designed based on the role of C-terminal residue, and its antihypertensive effects on spontaneously hypertensive rats
Bioactive peptides are formed by linking two or more proteinogenic amino acids via peptide bonds, typically ranging in len...
Design, synthesis, and antitumor activity of stapled peptide inhibitors targeting the RAS–RAF interactions
The RAS genes (KRAS, HRAS, and NRAS) are well-known oncogenes, and mutations in these genes can lead to uncontrolled cell ...
Synthesis of Benzo[h]quinoline derivatives and evaluation of their insecticidal activity against Culex pipiens L. larvae
Benzo[h]quinoline derivatives are valuable scaffolds found in pharmaceuticals and natural products, known for their divers...
Discovery of phenylisoxazolidine analogs targeting receptor interacting protein kinase 1 with anti-inflammatory activity
Necroptosis is a type of programmed cell death that was first proposed in 2005 and is associated with a variety of inflamm...
Structural optimization and discovery of high effective isopropanolamine-based TPS1 inhibitors as promising broad-spectrum fungicide candidates
Pathogenic fungi are one of the major culprits in causing plant diseases, posing a serious threat to the production of foo...
Elucidating the dual mechanistic action and synergism of platinum complexes bearing valproic acid as leaving ligand on NF-κB and inflammatory pathways in glioma
Gliomas, including glioblastomas, rank among the most prevalent and aggressive types of brain tumors [1]. Despite extensiv...
Fungal dimeric xanthones as anticancer agents by novelly stimulating sodium-calcium exchanger 1
Xanthone dimers (Xds) are widely derived from various species of fungi, plants and lichens [1]. Xds primarily consist of t...
Design, synthesis, and activity evaluation of novel STING inhibitors based on C170 and H151
The interferon gene-stimulating protein (STING) is a pivotal molecular target for regulating intrinsic immune function [1]...
Design, synthesis and preliminary structure-activity relationship of 2-iminothiazolidine-4-one derivatives against Schistosoma japonicum in vitro and in vivo
Schistosomiasis is an important prevalent disease in approximately 80 countries in tropical and subtropical regions, ranki...
Synthesis and identification of azocoumarin derivatives toward imaging of α-synuclein aggregates in the brain
α-Synuclein (α-syn) is an intrinsically disordered protein that accumulates and aggregates in Lewy bodies and Lewy neurite...
Discovery of environment-sensitive fluorescent ligands for SHP2 imaging in living cells and tumor sections
SHP2, a non-receptor tyrosine phosphatase belonging to the PTP family, plays a crucial role in cellular signal transductio...
TCM theory-inspired discovery of DNJ-flavonoid conjugates as broad-spectrum anti-SARS-CoV-2 agents by primarily targeting ER-associated glycoprotein folding process
The COVID-19 pandemic, caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has resulted in approximate...
Optimized ebselen derivatives as novel potent Escherichia coli β-glucuronidase covalent allosteric inhibitors
Gut microbiota is a complex microbial ecosystem that resides in the human intestine. Under normal physiological conditions...
Semisynthesis and biological evaluation of 17-hydroxybrevianamide N derivatives as anti-inflammatory agents by mediating NF-κB and MAPK signaling pathways
The maintenance of an inflammatory response is associated with the pathogenesis of chronic inflammatory diseases [1], incl...
Identification of novel diarylpyrimidine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against wild-type and K103N mutant viruses
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Discovery of novel third generation P-glycoprotein inhibitors bearing an azo moiety with MDR-reversing effect
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Synthesis, evaluation and mechanistic insights of novel IMPDH inhibitors targeting ESKAPEE bacteria
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Identification of novel and potent triazoles targeting CYP51 for antifungal: Design, synthesis, and biological study
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First fragment-based screening identifies new chemotypes inhibiting ERAP1-metalloprotease
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Discovery of sp3-rich diazatricycloundecanes as lysosomotropic autophagy inhibitors
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Design, synthesis and enzymatic inhibition evaluation of novel 4-hydroxy Pd–C-Ⅲ derivatives as α-glucosidase and PTP1B dual-target inhibitors
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Impact of site-specific conjugation strategies on the pharmacokinetics of antibody conjugated radiotherapeutics
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Adenanthin exhibits anti-inflammatory effects by covalently targeting the p65 subunit in the NF-κB signaling pathway
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Hit-to-lead optimization of 4,5-dihydrofuran-3-sulfonyl scaffold against Leishmania amazonensis. Effect of an aliphatic moiety
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