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Dual-action mitochondria-targeted prodrugs that both deplete mitochondrial glutathione and deliver a toxic payload to the matrix
Mitochondrial glutathione (mGSH) protects the organelle and the cell against reactive oxygen species (ROS), electrophilic ...
Discovery of HDM2004, a potent, selective and orally bioavailable HPK1 inhibitor for tumor immunotherapy
Hematopoietic progenitor kinase 1 (HPK1, also known as MAP4K1) is a serine/threonine kinase belonging to the Ste20-related...
Synthesis of β-d-C-galactopyranosyl compounds including constrained derivatives from clickable building blocks and evaluation as ligands for galectins
A set of nineteen C-galactopyranosyl ligands, which included constrained compounds based on a bicyclic trans-decalin type ...
Liposome-encapsulated iridium(III) complexes significantly enhance antitumor efficiency through immunogenic cell death to increase CD8+ T cells
Cervical cancer is a significant global health challenge, particularly in low- and middle-income countries where limited a...
Design and synthesis of c-Met/PARP dual-target inhibitors for the treatment of BRCA wild-type TNBC
The triple-negative breast cancer (TNBC) accounts for approximately 15% to 20% of all breast carcinomas with a worse progn...
Design, synthesis and preclinical evaluation of a tumor extracellular nucleotidase CD73 targeted theranostic radiotracer
Malignant tumors have become a significant public health challenge threatening human health. Although significant progress...
Optimization of triazole-based small molecule disruptors of the Aha1/Hsp90 complex that manifest potent activities
Recent structure-activity relationship (SAR) studies identified multiple Hsp90/Aha1 small molecule disruptors that manifes...
Advancing fibroblast activation protein inhibitors for targeted radioligand therapy: Strategies and innovations to increase tumor residence time
Targeted radioligand therapy (TRT) delivers radionuclides systemically via tumor-specific ligands, allowing precise tumor ...
Current landscape and therapeutic prospects of indole-azole hybrids for colorectal cancer treatment: A mini-review
Colorectal cancer (CRC) constitutes a formidable global health burden and ranks among the leading causes of cancer-related...
Discovery of a tetrahydrobenzothiophen-2-yl-pyrazolo[1,5-a]pyrimidine-3-carboxamide-based PROTAC as degrader of SARS-CoV-2 main protease
Targeted protein degradation has emerged as a new strategy in drug development, particularly in the anti-cancer field. Alt...
An AI-based approach accelerates the discovery of protein–protein interaction modulators targeting NCS-1
Drug repurposing is an efficient strategy to accelerate the identification of therapeutic compounds by finding new uses fo...
PROTAC-mediated degradation of peroxisomal d-aspartate oxidase: A novel strategy to modulate d-aspartate homeostasis for schizophrenia treatment
For many years, D-amino acids were considered minor contributors to biological processes compared with their L-enantiomers...
Discovery of 2-(methylamino)-5,6,7,8-tetrahydropyrido[4,3-d] pyrimidine derivatives as novel HsClpP activators for multiple myeloma therapy
Multiple myeloma (MM) is a cytogenetically heterogeneous clonal plasma cell proliferative disorder that accounts for appro...
Design and development of 1,5-diarylpyrazole-based multitarget-directed ligands as dual COX-2/HDAC6 inhibitors for Alzheimer's disease therapy: Molecular dynamics and experimental insights
Alzheimer's disease (AD), the most common form of dementia, is characterized by progressive neurodegeneration, memory loss...
Light-activated targeted degradation of VHL drug for selective tumor killing: A novel strategy for precision therapy of bladder cancer
Enhancing anticancer efficacy while avoiding toxicity to normal tissues represents a critical scientific challenge in anti...
Discovery of triazolyl azabicyclo[3.1.0]hexane derivative as an autotaxin inhibitors for the treatment of pulmonary fibrosis
Fibrosis is a pathological condition characterized by excessive deposition of extracellular matrix (ECM) proteins, leading...
Discovery of selective JAK1/2 inhibitor H018, a phase II agent with demonstrated preclinical anti-rheumatoid arthritis activity
Rheumatoid arthritis (RA) is a chronic, systemic, autoimmune inflammatory disorder that primarily targets the synovial joi...
Identification and optimization of first-in-class RNA helicase inhibitors of DDX1, LGP2, and MDA5
RNA helicases are essential, dynamic proteins that consume ATP to unwind and rearrange RNA. These activities place RNA hel...
Optimization of the fragment binding to hinge region for a potent PIM kinase inhibitor based on N-pyridinyl amide scaffold
Kinases are enzymes that transfer terminal phosphate group of the adenosine triphosphate (ATP) to specific substrate to re...
Phenoxy-linked colchicine derivatives: A structure-based approach toward enhanced selectivity and α-tubulin interaction
Cancer is a heterogeneous group of diseases marked by uncontrolled cell proliferation and metastasis, a major cause of can...
Medicinal chemistry approaches to the discovery and development of p300/CBP inhibitors for cancer therapy
The transcriptional coactivators p300 and CBP (CREB-binding protein) play a central role in gene regulation by functioning...
Methylenedioxy open-loop and closed-loop aporphines designed for the evaluation of potential antidepressants
For psychomodulators, some fragments in the chemical structures will play a decisive role in the regulation of certain key...
Rational design of NAMPT-based dual inhibitors with improved drug-like and pharmacokinetic properties for cancer treatment
Immunotherapy targeting the PD-1/PD-L1 axis has emerged as a transformative strategy in cancer treatment [1]. By reinvigor...
Structure-based design of benzofuran library as P. aeruginosa quorum sensing inhibitors: Synthesis, biological evaluation and molecular docking study
Antibiotics are widely used around the world for the treatment of infectious diseases. The hysterical use of antibiotics l...
Targeting voltage-gated proton channel HV1: Optimised 5-phenyl-2-aminoimidazoles with anticancer potential
The voltage-gated proton channel (HV1) has been linked to the development of tumours, neuroinflammatory diseases, immune d...
CHI3L1-targeted small molecules as glioblastoma therapies: Virtual screening-based discovery, biophysical validation, pharmacokinetic profiling, and evaluation in glioblastoma spheroids
Among brain tumors, glioblastoma (GBM) is widely recognized as the most aggressive and lethal primary brain malignancy whi...
Discovery of a novel and potent antiplatelet thiol prodrug CG-0255
Cardiovascular and cerebrovascular diseases remain the leading cause of deaths worldwide with nearly half of the deaths be...
An optimized 2,2′-dipicolylamine-rutaecarpine quaternary ammonium derivative: targeting bacterial membrane disruption for enhanced anti-methicillin-resistant Staphylococcus aureus (MRSA) activity
Antimicrobial resistance (AMR) is widely recognized as one of the most significant threats to global public health, result...
Bioactive sesquiterpene lactones from Elephantopus scaber: semi-synthesis, target fishing, anti-malignant glioma efficacy in vitro and in vivo
Malignant glioma (MG), a highly aggressive tumor in the central nervous system (CNS), is marked by rapid cell proliferatio...
Targeting α4β1 integrin: from cyclic to linear ligands, effects of chemical modifications
The immune system depends on integrins for adhesion and migration during leukocyte trafficking and for intracellular signa...
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